Pesticidal pyridinecarboxamide derivatives

ABSTRACT

The invention relates to 3-pyridylcarboxamide derivatives of formula (I): 
                         
wherein the various symbols are as defined in the description, compositions thereof, methods for controlling pests by applying same, and processes for their preparation.

CROSS-REFERENCE TO RELATED APPLICATIONS

This application is the U.S. national stage of International Appln. No.PCT/EP03/04715, filed May 6, 2003, and claims priority under 35 U.S.C. §119(a)-(d) of European Patent Application No. 02010911.2, filed May 16,2002, said applications being incorporated by reference herein in theirentireties and relied upon.

The invention relates to 3-pyridylcarboxamide derivatives and their usefor the control of pests, in particular arthropods such as insects andacarids, and helminths (including nematodes); to compositions containingthem, and to processes and intermediates for their preparation.

The control of insects, nematodes or helminths with 3-pyridylcarboxamidecompounds has been described in many patents such as EP 580374, JP10101648, JP 10182625, WO 200109104, WO 200114340, JP 6321903, JP10195072 and JP 11180957.

However, the level of action and/or duration of action of theseprior-art compounds is not entirely satisfactory in all fields ofapplication, in particular against certain organisms or when lowconcentrations are applied.

Since modern pesticides must meet a wide range of demands, for exampleregarding level, duration and spectrum of action, use spectrum,toxicity, combination with other active substances, combination withformulation auxiliaries or synthesis, and since the occurrence ofresistances is possible, the development of such substances can never beregarded as concluded, and there is constantly a high demand for novelcompounds which are advantageous over the known compounds, at least asfar as some aspects are concerned.

It is an object of the present invention to provide compounds whichwiden the spectrum of the pesticides in various aspects.

The present invention provides a compound which is a3-pyridylcarboxamide derivative of formula (I):

wherein:

-   N=Q is a formula (A) or (B):

-   Z is YR¹ or NR⁵R⁶;-   or when Z is YR¹, R¹ and R³ may form together with the adjacent    —Y—C—NR²— atoms, a five or six membered saturated heterocyclic ring    which optionally contains an additional N or O atom, and is    unsubstituted or substituted by one or more R⁷ groups or one of the    ring carbon atoms may form a carbonyl or imino group, and which ring    is optionally fused to a benzene ring optionally substituted by R⁷;-   or when Z is YR¹, R¹ and R³ may form together with the adjacent    —Y—C—NR²— atoms, a group (A²):

-   Y, X and W are each independently O or S;-   or R¹ and R⁴ may form together with the adjacent —X—C—W— group, a    five or six membered unsaturated, partially saturated or saturated    heterocyclic ring, unsubstituted or substituted by one or more R⁷    groups or one of the ring carbon atoms may form a carbonyl group;-   R¹ is (C₁-C₈)alkyl, (C₃-C₆)alkenyl, (C₃-C₆)alkynyl or    (C₃-C₈)cycloalkyl, which last four mentioned groups are    unsubstituted or substituted by one or more R⁸ groups; or is    (C₃-C₈)cycloalkyl-(C₁-C₆)alkyl which cycloalkyl is unsubstituted or    substituted by one or more R⁸ groups; or is —(CR⁹R¹⁰)_(p)R¹¹ or    —(CR⁹R¹⁰)_(p)heterocyclyl; or when Y is O is (C₁-C₆)alkylamino,    NH(C₃-C₈)cycloalkyl or NH(CH₂)_(n)R¹¹;-   R^(2a) is (C₁-C₈)alkyl, (C₃-C₆)alkenyl, (C₃-C₆)alkynyl,    (C₃-C₈)cycloalkyl, (C₁-C₆)alkoxy, (C₃-C₆)alkenyloxy,    (C₃-C₆)alkynyloxy, (C₁-C₆)alkylamino, di-(C₁-C₆)alkylamino,    NHCO(C₁-C₆)alkyl, NHSO₂(C₁-C₆)alkyl, CO(C₁-C₆)alkyl or    SO₂(C₁-C₆)alkyl which last thirteen mentioned groups are    unsubstituted or substituted by one or more R⁸ groups; or is    (C₃-C₈)cycloalkyl-(C₁-C₆)alkyl which cycloalkyl is unsubstituted or    substituted by one or more R⁸ groups; or is —(CR⁹R¹⁰)_(p)R¹¹,    —(CR⁹R¹⁰)_(p)heterocyclyl, OH, SO₂R¹¹, NH₂, NHCOR¹¹, NHR¹¹,    NH(C₃-C₈)cycloalkyl, NH(CH₂)_(s)R¹¹, O(CHR¹⁰)_(r)R¹¹;    O(CH₂)_(r)heterocyclyl or N═C[(C₁-C₆)alkyl]₂; or is (C₃-C₆)alkenyl    substituted by R¹¹;-   R² and R⁵ are each independently R², or H;-   R³ and R⁶ are each independently H or R¹;-   R⁴ is (C₁-C₆)alkyl substituted by R⁸; or is (C₃-C₆)alkenyl,    (C₃-C₆)alkynyl or (C₃-C₈)cycloalkyl which last three mentioned    groups are unsubstituted or substituted by one or more R⁸ groups; or    is (C₃-C₈)cycloalkyl-(C₁-C₆)alkyl unsubstituted or substituted by    one or more R⁸ groups; or is —(CR⁹R¹⁰)_(p)R¹¹ or    —(CR⁹R¹⁰)_(p)heterocyclyl;-   or when W is O, R⁴ is (C₁-C₆)alkylamino;-   or R² and R³ together with the adjacent N atom form a 3 to    8-membered unsaturated, partially saturated or saturated    heterocyclic ring which optionally contains up to three additional    N, O or S atoms and which ring is unsubstituted or substituted by    one or more R⁷ groups (preferred examples of such ring systems    include pyrrolidin-1-yl, piperidin-1-yl, 4,5-dihydropyrazol-1-yl,    morpholin-1-yl, thiomorpholin-1-yl or its S-oxide or S, S-dioxide);-   R⁷ is R⁸, R⁴, (C₁-C₆)alkyl or CH₂OH;-   R⁸ is halogen, (C₁-C₅)alkoxy, (C₁-C₆)haloalkoxy, S(O)_(n)R¹², CN,    CO₂(C₁-C₆)alkyl, CO₂H, NO₂, OH, amino, (C₁-C₆)alkylamino,    di-(C₁-C₆)alkylamino, carbamoyl, (C₁-C₆)-alkylcarbamoyl,    di-(C₁-C₆)-alkylcarbamoyl, CH[O(C₁-C₆)alkyl]₂, (C₃-C₆)alkenyloxy,    (C₃-C₆)alkynyloxy or O(CH₂)_(r)R¹¹;-   R⁹ and R¹⁰ are each independently H, (C₁-C₆)alkyl or    (C₁-C₆)haloalkyl;-   R¹¹ is aryl unsubstituted or substituted by one or more groups    selected from (C₁-C₆)alkyl, (C₁-C₆)haloalkyl, (C₂-C₆)alkenyl,    (C₂-C₆)alkynyl, (C₃-C₈)cycloalkyl, —(CH₂)_(u)R¹³, heterocyclyl,    halogen, (C₁-C₆)alkoxy, (C₁-C₆)haloalkoxy, S(O)_(n)R¹², CN,    CO₂(C₁-C₆)alkyl, NO₂, amino, (C₁-C₆)alkylamino and    di-(C₁-C₆)alkylamino;-   R¹² is (C₁-C₆)alkyl or (C₁-C₆)haloalkyl;-   R¹³ is phenyl unsubstituted or substituted by one or more groups    selected from halogen, (C₁-C₆)alkyl and (C₁-C₆)haloalkyl;-   R^(e) is H, (C₁-C₆)alkyl, (C₂-C₆)alkenyl, (C₂-C₆)alkynyl,    (C₃-C₈)cycloalkyl, (C₃-C₈)cycloalkyl-(C₁-C₆)alkyl, halogen,    (C₁-C₆)alkoxy, (C₁-C₆)haloalkoxy, S(O)_(n)R¹², (C₃-C₆)alkenyloxy,    (C₃-C₆)alkynyloxy, —(CH₂)_(p)R¹¹, heterocyclyl, CN, CO₂(C₁-C₆)alkyl,    NO₂, amino, (C₁-C₆)alkylamino, di-(C₁-C₆)alkylamino or O(CH₂)_(r)R¹¹    wherein r is 0 or 1;-   U is N or CH,-   m, s and u are each independently 0 or 1;-   n is 0, 1 or 2;-   p is 0, 1, 2 or 3;-   r is 0 or an integer from 1 to 6; and each heterocyclyl in the above    mentioned radicals is independently a mono or bicyclic heterocyclic    radical having 3 to 7 ring atoms in each ring and 1 to 4 hetero    atoms selected from N, O and S;-   with the proviso that in (A) when Z is NR⁵R⁶ then up to three of R²,    R³, R⁵ and R⁶ are not simultaneously H;-   or a pesticidally acceptable salt thereof.

These compounds possess valuable pesticidal properties.

The invention also encompasses any stereoisomer, enantiomer or geometricisomer, and mixtures thereof.

By the term “pesticidally acceptable salts” is meant salts the cationsor anions of which are known and accepted in the art for the formationof salts for pesticidal or horticultural use. Suitable salts with bases,e.g. formed by compounds of formula (I) containing a carboxy or OHgroup, include alkali metal (e.g. sodium and potassium), alkaline earthmetal (e.g. calcium and magnesium), ammonium and amine (e.g.diethanolamine, triethanolamine, octylamine, morpholine anddioctylmethylamine) salts. Suitable acid addition salts, e.g. formed bycompounds of formula (I) containing an amino group, include salts withinorganic acids, for example hydrochlorides, sulphates, phosphates andnitrates and salts with organic acids for example acetic acid.

In the present patent specification, including the accompanying claims,the aforementioned substituents have the following meanings:

-   halogen atom means fluorine, chlorine, bromine or iodine;-   alkyl groups and portions thereof (unless otherwise defined) may be    straight- or branched-chain;-   cycloalkyl groups preferably have from three to six carbon atoms in    the ring and are optionally substituted by halogen or alkyl.

The haloalkyl and haloalkoxy groups bear one or more halogen atoms;preferred groups of this type include —CF₃ and —OCF₃.

The term “halo” before the name of a radical means that this radical ispartially or completely halogenated, that is to say, substituted by F,Cl, Br, or I, in any combination, preferably by F or Cl.

The expression “(C₁-C₆)-alkyl” is to be understood as meaning anunbranched or branched hydrocarbon radical having 1, 2, 3, 4, 5 or 6carbon atoms, such as, for example a methyl, ethyl, propyl, isopropyl,1-butyl, 2-butyl, 2-methylpropyl or tert-butyl radical.

“(C₁-C₆)-Haloalkyl” is to be understood as meaning an alkyl groupmentioned under the expression “(C₁-C₆)-alkyl” in which one or morehydrogen atoms are replaced by the same number of identical or differenthalogen atoms, preferably by chlorine or fluorine, such as thetrifluoromethyl, the 1-fluoroethyl, the 2,2,2-trifluoroethyl, thechloromethyl, fluoromethyl, the difluoromethyl or the1,1,2,2-tetrafluoroethyl group.

“(C₁-C₆)-Alkoxy” is to be understood as meaning an alkoxy group whosehydrocarbon radical has the meaning given under the expression“(C₁-C₆)-alkyl”.

The terms “alkenyl” and “alkynyl” with a range of carbon atoms stated asprefix denote a straight-chain or branched hydrocarbon radical having anumber of carbon atoms which corresponds to this stated range and whichcontains at least one multiple bond which can be located in any positionof the respective unsaturated radical. “(C₂-C₆)-Alkenyl” accordinglydenotes, for example, the vinyl, allyl, 2-methyl-2-propenyl, 2-butenyl,pentenyl, 2-methylpentenyl or the hexenyl group. “(C₂-C₆)-Alkynyl”denotes, for example, the ethynyl, propargyl, 2-methyl-2-propynyl;2-butynyl; 2-pentynyl or the 2-hexynyl group.

“(C₃-C₈)-Cycloalkyl” denotes monocyclic alkyl radicals, such as thecyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl orcyclooctyl radical, and denotes bicyclic alkyl radicals, such as thenorbornyl radical.

The expression “(C₃-C₈)-cycloalkyl-(C₁-C₆)-alkyl” is to be understood asmeaning, for example the cyclopropylmethyl, cyclopentylmethyl,cyclohexylmethyl, cyclohexylethyl, cyclohexylbutyl, 1-methylcyclopropyl,1-methylcyclopentyl, 1-methylcyclohexyl, 3-hexylcyclobutyl or the4-tert-butylcyclohexyl radical.

“(C₁-C₆)-Alkylamino” denotes a nitrogen atom which is substituted by analkyl radical of the above definition. “Di-(C₁-C₆)-alkylamino” denotes anitrogen atom which is substituted by two alkyl radical of the abovedefinition.

The expression “(C₁-C₆)-alkylcarbamoyl” denotes a carbamoyl group havingone hydrocarbon radical which has the meaning given under the expression“(C₁-C₆)-alkyl”; and “di-(C₁-C₆)-alkylcarbamoyl” denotes a carbamoylgroup having two hydrocarbon radicals which can be identical ordifferent.

The expression “aryl” is to be understood as meaning a carbocyclic, i.e.constructed of carbon atoms, aromatic radical having preferably 6 to 14,in particular 6 to 12, carbon atoms, such as, for example, phenyl,naphthyl or biphenylyl, preferably phenyl.

The expression “heterocyclyl” preferably denotes a cyclic radical whichcan be completely saturated, partially unsaturated or completelyunsaturated and which contains in the ring one or more identical ordifferent atoms selected from the group consisting of nitrogen, sulfurand oxygen, where, however, two oxygen atoms may not be directlyadjacent and at least one carbon atom has to be present in the ring,such as, for example, a thiophene, furan, pyrrole, thiazole, oxazole,imidazole, isothiazole, isoxazole, pyrazole, 1,3,4-oxadiazole,1,3,4-thiadiazole, 1,3,4-triazole, 1,2,4-oxadiazole, 1,2,4-thiadiazole,1,2,4-triazole, 1,2,3-triazole, 1,2,3,4-tetrazole, benzo[b]thiophene,benzo[b]furan, indole, benzo[c]thiophene, 1,3-benzodioxole,1,3-benzodioxane, benzo[c]furan, isoindole, benzoxazole, benzothiazole,benzimidazole, benzisoxazole, benzisothiazole, benzopyrazole,benzothiadiazole, benzotriazole, dibenzofuran, dibenzothiophene,carbazole, pyridine, pyrazine, pyrimidine, pyridazine, 1,3,5-triazine,1,2,4-triazine, 1,2,4,5-tetrazine, quinoline, isoquinoline, quinoxaline,quinazoline, cinnoline, 1,8-naphthyridine, 1,5-naphthyridine,1,6-naphthyridine, 1,7-naphthyridine, phthalazine, pyridopyrimidine,purine, pteridine, 4H-quinolizine, piperidine, pyrrolidine, oxazoline,tetrahydrofuran, tetrahydropyran, isoxazolidine, thiazolidine, oxiraneor oxetane radical.

Heterocyclyl preferably denotes a saturated, partially saturated oraromatic ring system having 3 to 7 ring atoms and 1 to 4 heteroatomsselected from the group consisting of O, S and N, where at least onecarbon atom has to be present in the ring.

More preferably, heterocyclyl denotes a pyridine, pyrimidine,(1,2,4)-oxadiazole, (1,3,4)-oxadiazole, pyrrole, furan, thiophene,oxazole, thiazole, imidazole, pyrazole, isoxazole, 1,2,4-triazole,tetrazole, pyrazine, pyridazine, oxazoline, thiazoline, tetrahydrofuran,tetrahydropyran, morpholine, piperidine, piperazine, pyrroline,pyrrolidine, oxazolidine, thiazolidine, oxirane, oxetane,1,3-benzodioxole or 1,3-benzodioxane radical.

Preferred substituents for the various aliphatic, aromatic andheterocyclic ring systems include halogen, nitro, cyano, (C₁-C₄)-alkyl,(C₃-C₆)-cycloalkyl, (C₁-C₄)-alkoxy, (C₁-C₄)-alkylthio,(C₁-C₄)-alkylsulfinyl, (C₁-C₄)-alkylsulfonyl, phenyl, benzyl andphenoxy, where in the alkyl radicals and the radicals derived therefromone or more—and in the case of fluorine up to the maximum numberof—hydrogen atoms can be replaced by halogen, preferably chlorine orfluorine.

Particularly preferred substituents include halogen, nitro, cyano,(C₁-C₄)-alkyl, (C₁-C₄)-haloalkyl, (C₃-C₆)-cycloalkyl, (C₁-C₄)-alkoxy,(C₁-C₄)-haloalkoxy, (C₁-C₄)-alkylthio and (C₁-C₄)-haloalkylthio.

It is to be generally understood, unless otherwise stated, that the term“unsubstituted or substituted by one or more groups” or “unsubstitutedor substituted by one or more groups selected from” means that suchgroups (or preferred groups) may be the same or different.

The term pests means arthropod pests (including insects and acarids),and helminths (including nematodes).

Preferably Z is YR¹;

-   or preferably when Z is YR¹, R¹ and R³ may form together with the    adjacent —Y—C—NR²— atoms, a five or six membered saturated    heterocyclic ring which optionally contains an additional N or O    atom, and is unsubstituted or substituted by one or more R⁷ groups    or one of the ring carbon atoms may form a carbonyl or imino group,    and which ring is optionally fused to a benzene ring optionally    substituted by R⁷; preferably one of X and W is O and the other is    S;-   or preferably R¹ and R⁴ may form together with the adjacent —X—C—W—    group, a five or six membered unsaturated, partially saturated or    saturated heterocyclic ring, unsubstituted or substituted by one or    more R⁷ groups or one of the ring carbon atoms may form a carbonyl    group.

Preferably R¹ is (C₁-C₈)alkyl or (C₃-C₆)alkenyl, which groups areunsubstituted or substituted by one or more groups selected from(C₁-C₄)alkoxy, S(O)_(n)R¹² and OH; or is —(CR⁹R¹⁰)_(p)R¹¹ (morepreferably R¹ is (C₁-C₈)alkyl, (C₃-C₆)alkenyl or —(CR⁹R¹⁰)_(p)R¹¹).

Preferably R² is H, (C₃-C₆)alkenyl, (C₃-C₆)alkynyl, (C₁-C₆)alkoxy,(C₃-C₆)alkenyloxy, (C₃-C₆)alkynyloxy, —(CR⁹R¹⁰)_(p)R¹¹,—(CR⁹R¹⁰)_(p)heterocyclyl, NHR¹¹ or O(CH₂)_(r)R¹¹; or is (C₁-C₈)alkylunsubstituted or substituted by a di-(C₁-C₄)alkylamino group; (morepreferably R² is (C₁-C₈)alkyl, (C₃-C₆)alkenyl, (C₁-C₆)alkoxy,—(CR⁹R¹⁰)_(p)R¹¹, —(CR⁹R¹⁰)_(p)heterocyclyl or O(CH₂)_(r)R¹¹).

Preferably R³ is (C₁-C₈)alkyl or (C₃-C₆)alkenyl, which groups areunsubstituted or substituted by an (C₁-C₄)alkoxy or OH group; or is H or—(CR⁹R¹⁰)_(p)R¹¹ (more preferably R³ is H, (C₁-C₈)alkyl, (C₃-C₆)alkenylor —(CH₂)_(n)R¹¹).

Preferably R⁴ is (C₁-C₈)alkyl substituted by (C₁-C₄)alkoxy or OH; or is(C₃-C₆)alkenyl, (C₃-C₆)alkynyl or (C₃-C₈)cycloalkyl which last threementioned groups are unsubstituted or substituted by an (C₁-C₄)alkoxy orOH group; or is (C₃-C₈)cycloalkyl-(C₁-C₆)alkyl which cycloalkyl isunsubstituted or substituted by an (C₁-C₄)alkoxy or OH group; or is—(CR⁹R¹⁰)_(p)R¹¹ or —(CR⁹R¹⁰)_(p)heterocyclyl (more preferably R⁴ is(C₁-C₈)alkyl, (C₃-C₆)alkenyl or —(CH₂)_(p)phenyl);

-   or preferably R² and R³ together with the adjacent N atom form a 3    to 8-membered unsaturated, partially saturated or saturated    heterocyclic ring which optionally contains up to three additional    N, O or S atoms and which ring is unsubstituted or substituted by    one or more R⁷ groups (preferred examples of such ring systems    include pyrrolidin-1-yl, piperidin-1-yl, morpholin-1-yl,    thiomorpholin-1-yl or 4,5-dihydropyrazol-1-yl).

Preferably R⁷ is (C₁-C₄)alkoxy, OH, R⁴, (C₁-C₄)alkyl or CH₂OH.

Preferably R⁸ is (C₁-C₄)alkoxy or OH.

Preferably R⁹ and R¹⁰ which may be the same or different, are eachindependently selected from H, (C₁-C₄)alkyl and (C₁-C₄)haloalkyl.

Preferably R¹¹ is phenyl unsubstituted or substituted by one or moregroups selected from (C₁-C₄)alkyl, (C₁-C₄)haloalkyl, (C₂-C₄)alkenyl,(C₂-C₄)alkynyl, (C₃-C₆)cycloalkyl, —(CH₂)_(u)R¹³, heterocyclyl, halogen,(C₁-C₄)alkoxy, (C₁-C₄)haloalkoxy, S(O)_(n)R¹², CN, CO₂(C₁-C₄)alkyl, NO₂,amino, (C₁-C₄)alkylamino and di-(C₁-C₄)alkylamino; (more preferably R¹¹is phenyl unsubstituted or substituted by one or more groups selectedfrom (C₁-C₄)alkyl, halogen, (C₁-C₄)alkoxy, NO₂ and amino).

Preferably R¹² is (C₁-C₄)alkyl or (C₁-C₄)haloalkyl.

Preferably m is 0.

Preferably p, r, s and u are each independently 0 or 1.

Preferably each heterocyclyl in the above mentioned radicals isindependently a heterocyclic radical having 3 to 7 ring atoms and 1 to 4hetero atoms selected from N, O and S;

A preferred embodiment of the invention comprises compounds of formula(I) wherein N=Q is a formula (A) in which Z is YR¹ and R¹ and R³ formtogether with the adjacent —Y—C—NR²— atoms, a heterocyclic ring which isof formula (A¹), (A²), (A³) or (A⁴):

wherein:

-   Y is O or S;-   U is N or CH;-   V is O or CH₂;-   t is 0 or 1;-   R^(a), R^(b), R^(c) and R^(d) are each independently selected from    H, (C₁-C₆)alkyl, (C₁-C₆)haloalkyl, (C₂-C₆)alkenyl, (C₂-C₆)alkynyl,    (C₃-C₈)cycloalkyl, halogen, (C₁-C₆)alkoxy, (C₁-C₆)haloalkoxy,    S(O)_(n)R¹² (C₂-C₆)alkenyloxy, (C₂-C₆)alkynyloxy, R¹¹, heterocyclyl    and O(CH₂)_(r)R¹¹ wherein r is 0 or 1;-   or R^(a) and R^(b), or R^(c) and R^(d) may form a carbonyl or imino    group (more preferably R^(a), R^(b), R^(c) and R^(d) are each    independently selected from H, (C₁-C₆)alkyl, (C₁-C₆)alkoxy and R¹¹;    or R^(a) and R^(b), or R^(c) and R^(d) may form a carbonyl or imino    group; most preferably R^(a), R^(b), R^(c) and R^(d) are each H or    R^(c) and R^(d) form a carbonyl group, or R^(a) and R^(b) form an    imino group);-   R^(e) and R^(f) are each independently selected from H,    (C₁-C₆)alkyl, (C₂-C₆)alkenyl, (C₂-C₆)alkynyl, (C₃-C₈)cycloalkyl,    (C₃-C₈)cycloalkyl-(C₁-C₆)alkyl, halogen, (C₁-C₆)alkoxy,    (C₁-C₆)haloalkoxy, S(O)R¹² (C₂-C₆)alkenyloxy, (C₂-C₆)alkynyloxy,    —(CH₂)_(p)R¹¹, heterocyclyl, CN, CO₂(C₁-C₆)alkyl, NO₂, amino,    (C₁-C₆)alkylamino, di-(C₁-C₆)alkylamino and O(CH₂)_(n)R¹¹ wherein r    is 0 or 1 (more preferably R^(e) and R^(f) are each independently    selected from H, (C₁-C₆)alkyl, (C₁-C₆)haloalkyl, halogen and R¹¹;    most preferably R^(e) and R^(f) are each H);-   R^(g) is H, (C₁-C₆)alkyl, halogen, (C₁-C₆)alkoxy, CO₂(C₁-C₆)alkyl or    R¹¹ (more preferably R^(g) is H);-   R^(2a) is (C₁-C₆)alkyl unsubstituted or substituted by one or more    groups selected from halogen, (C₁-C₆)alkoxy, CH[O(C₁-C₆)alkyl]₂, CN,    CO₂(C₁-C₆)alkyl and CO₂H; or is (C₃-C₆)alkenyl unsubstituted or    substituted by one or more halogen or phenyl groups; or is    (C₃-C₆)alkynyl, (C₃-C₈)cycloalkyl, (C₃-C₈)cycloalkyl-(C₁-C₆)alkyl,    (C₁-C₆)alkoxy, (C₃-C₆)alkenyloxy or (C₃-C₆)alkynyloxy; or is    —(CHR¹⁰)_(p)R¹¹ wherein R¹⁰ is H or (C₁-C₈)alkyl, p is 0 or 1 and    R¹¹ is phenyl unsubstituted or substituted by one or more groups    selected from halogen, (C₁-C₆)haloalkyl, (C₁-C₆)alkoxy,    (C₁-C₆)haloalkoxy and phenoxy unsubstituted or substituted by one or    more groups selected from halogen and (C₁-C₆)haloalkyl; or is    O(CHR¹⁰)_(r)R¹¹ wherein R¹⁰ is H or (C₁-C₆)alkyl, r is 1 and R¹¹ is    phenyl unsubstituted or substituted by one or more groups selected    from (C₁-C₆)haloalkyl, (C₁-C₆)alkoxy and NO₂; (more preferably    R^(2a) is (C₁-C₆)alkyl, (C₂-C₆)alkenyl or CH₂phenyl; or phenyl    unsubstituted or substituted by one or more halogen or    (C₁-C₆)haloalkyl groups; or is (C₂-C₆)alkenyl unsubstituted or    substituted by a phenyl group; or is CH₂CO₂H or CH₂CO₂(C₁-C₆)alkyl);    and-   R² is R^(2a) or H (more preferably R² is H, (C₁-C₆)alkyl,    (C₃-C₆)alkenyl, (C₁-C₆)alkoxy or CH₂phenyl; or is phenyl    unsubstituted or substituted by one or more halogen or    (C₁-C₆)haloalkyl groups; or is (C₃-C₆)alkenyl unsubstituted or    substituted by a phenyl group; or is CH₂CO₂H or CH₂CO₂(C₁-C₆)alkyl);    most preferably R² is H, (C₁-C₆)alkyl, (C₃-C₆)alkenyl,    (C₁-C₆)alkoxy, CH₂phenyl or phenyl).

A further preferred embodiment of the invention comprises compounds offormula (I) wherein N=Q is a formula (B) in which R¹ and R⁴ formtogether with the adjacent —X—C—W— group, a heterocyclic ring of formula(B¹) or (B²):

wherein:

-   R^(h), R^(i) and R^(j) are each independently H, (C₁-C₆)alkyl,    halogen, (C₁-C₆)alkoxy, CO₂(C₁-C₆)alkyl or R¹¹ (more preferably    R^(h), R^(i) and R^(j) are each independently H or (C₁-C₆)alkyl).

A more preferred class of compounds of formula (I) are of formula (Ia):

wherein R¹ is (C₃-C₆)alkenyl, (C₃-C₆)haloalkenyl, (C₃-C₆)alkynyl or(C₃-C₈)cycloalkyl-(C₁-C₆)alkyl; or is (C₁-C₆)alkyl unsubstituted orsubstituted by one or more CO₂(C₁-C₆)alkyl or CH[O(C₁-C₆)alkyl]₂ groups;or is —(CHR¹⁰)R¹¹ wherein R¹⁰ is H or (C₁-C₆)alkyl, and R¹¹ is phenylunsubstituted or substituted by one or more halogen or (C₁-C₆)haloalkylgroups;

-   R² is (C₁-C₆)alkyl, phenyl or N═C[(C₁-C₆)alkyl]₂; or is CH₂R¹¹ where    R¹¹ is phenyl unsubstituted or substituted by one or more halogen    groups; and-   R³ is H, (C₁-C₆)alkyl or phenyl; or R² and R³ together with the    adjacent N atom form a pyrrolidin-1-yl, piperidin-1-yl or    morpholin-1-yl ring.

A more preferred class of compounds of formula (I) are of formula (Ib):

wherein R¹ is (C₁-C₆)alkyl unsubstituted or substituted by a S(O)_(n)R¹²group;

-   R² is (C₃-C₆)alkenyl, (C₃-C₆)alkynyl, (C₃-C₈)cycloalkyl,    (C₃-C₈)cycloalkyl-(C₁-C₆)alkyl, (C₁-C₆)alkoxy or (C₃-C₆)alkenyloxy;    or is (C₁-C₈)alkyl unsubstituted or substituted by one or more    groups selected from halogen, (C₁-C₆)alkoxy, di-(C₁-C₆)alkylamino,    CN, CH[O(C₁-C₆)alkyl]₂, phenyl and phenoxy; or is NHR¹¹ wherein R¹¹    is phenyl unsubstituted or substituted by one or more    (C₁-C₆)haloalkyl groups; or is —(CHR¹⁰)R¹¹ wherein R¹⁰ is H or    (C₁-C₆)alkyl, and R¹¹ is phenyl unsubstituted or substituted by one    or more halogen, (C₁-C₆)alkyl or (C₁-C₆)haloalkyl groups; or is    —CH₂heterocyclyl wherein heterocyclyl is thienyl, pyridyl, furyl or    1,3-benzodioxolanyl; or is OCH₂heterocyclyl wherein heterocyclyl is    benzo-1,3-dioxanyl unsubstituted or substituted by one or more    halogen groups; and-   R³ is H or (C₁-C₆)alkyl.

A more preferred class of compounds of formula (I) are of formula (Ic):

wherein R¹ is (C₃-C₆)alkenyl or (C₃-C₆)alkynyl; or is —(CHR¹⁰)R¹¹wherein R¹⁰ is (C₁-C₆)alkyl, and R¹¹ is phenyl unsubstituted orsubstituted by one or more (C₁-C₆)haloalkyl groups; and

-   R⁴ is (C₁-C₆)alkylamino; or is (C₁-C₆)alkyl unsubstituted or    substituted by one or two (C₁-C₆)alkoxy or S(O)_(n)R¹² groups.

A more preferred class of compounds of formula (I) are those in whichN=Q is a formula (A¹) above, wherein:

-   R^(a) and R^(b) are each H or (C₁-C₆)alkyl, or R^(a) and R^(b) form    an imino group; R^(c) is H, (C₁-C₆)alkyl, (C₁-C₆)alkoxy or phenyl;    R^(d) is H or (C₁-C₆)alkyl; or R^(a) and R^(b) or R^(c) and R^(d)    may form a carbonyl group;-   Y is O or S; and-   R² is H, (C₁-C₆)alkyl or CH₂phenyl; or phenyl unsubstituted or    substituted by one or more halogen groups; or (C₃-C₆)alkenyl    substituted by phenyl.

A further more preferred class of compounds of formula (I) are those inwhich N=Q is a formula (A²) above, wherein:

-   R^(e) is H, (C₁-C₆)alkyl, (C₁-C₆)haloalkyl or phenyl;-   U is N or CH; and-   R^(2a) is (C₁-C₆)alkyl, CH₂CO₂H, CH₂CO₂(C₁-C₆)alkyl or CH₂phenyl; or    is phenyl unsubstituted or substituted by one or more    (C₁-C₆)haloalkyl groups; or is (C₃-C₆)alkenyl unsubstituted or    substituted by a phenyl group.

A further more preferred class of compounds of formula (I) are those inwhich N=Q is a formula (A³) above, wherein:

-   R^(f) is H or halogen;-   t is 0 or 1; and-   R² is H, (C₃-C₆)alkenyl or CH₂phenyl.

A further more preferred class of compounds of formula (I) are those inwhich N=Q is a formula (A⁴) above, wherein:

-   R^(g) is H;-   Y is O or S;-   V is O or CH₂; and-   R² is H.

The compounds of general formula (I) can be prepared by the applicationor adaptation of known methods (i.e. methods heretofore used ordescribed in the chemical literature.

In the following description of processes when symbols appearing informulae are not specifically defined, it is understood that they are“as defined above” in accordance with the first definition of eachsymbol in the specification.

According to a feature of the invention compounds of formula (I) whereinN=Q is a formula (A) in which Z is YR¹, m is zero, and R¹, R² and R³ areas defined above, may be prepared by the reaction of a compound offormula (II):

wherein Y, R² and R³ are as defined above, with a compound of formula(III):R¹L  (III)wherein R¹ is as defined above and L is a leaving group generallyhalogen and preferably chlorine or bromine. The reaction is generallyperformed in the presence of an organic base such as a tertiary aminefor example triethylamine, or pyridine, or an inorganic base such as analkali metal carbonate, for example potassium carbonate, or an alkalimetal alkoxide such as sodium ethoxide, or sodium hydride, in a solventsuch as dioxan, tetrahydrofuran or N,N-dimethylformamide, at atemperature of from 0° to 100° C. (preferably 0° to 50° C.).

According to a further feature of the invention compounds of formula (I)wherein N=Q is a formula (A) in which Z is YR¹, m is zero, R³ is H, andR¹ and R² are as defined above, may be prepared in a 1-pot process bythe reaction of a compound of formula (IV):

with a strong base such as sodium hydride, and an isothiocyanate orisocyanate compound of formula (V):R²—N═C═Y  (V)wherein R² is as defined above, in an inert solvent such asN,N-dimethylformamide, at a temperature of from 0° to 60° C., to givethe corresponding acylthiourea or acylurea intermediate of formula (II)above wherein R³ is H, which is generally not isolated, and is reactedwith a compound of formula (III) as described above. The reaction isgenerally performed in an inert solvent such as N,N-dimethylformamide ata temperature of from 0° to 60° C.

According to a further feature of the invention compounds of formula (I)wherein N=Q is a formula (A) which is a heterocyclic ring of formula(A¹), (A²), (A³) or (A⁴), wherein the various symbols are as definedabove, may be prepared by the acylation of the corresponding compound offormula (A^(1a)), (A^(2a)), (A^(3a)) or (A^(4a)):

wherein the various symbols are as defined above, with a compound offormula (VI):

wherein L is a leaving group, generally halogen and preferably chlorine.The reaction is generally performed in a solvent such asdichloromethane, at a temperature of from 0° to 100° C. (preferably 0°to 50° C.).

According to a further feature of the invention compounds of formula (I)wherein N=Q is a formula (A) in which Z is NR⁵R⁶, m is zero, and R², R³,R⁵ and R⁶ are as defined above, may be prepared by the reaction of acompound of formula (VII):

wherein R¹, R² and R³ are as defined above, with a compound of formula(VIII):HNR⁵R⁶  (VIII)wherein R⁵ and R⁶ are as defined above. The reaction is generallyperformed in the presence of an organic base such as a tertiary aminefor example triethylamine, or pyridine, or an inorganic base such as analkali metal carbonate, for example potassium carbonate, or an alkalimetal alkoxide such as sodium ethoxide, or sodium hydride, in a solventsuch as dioxan, tetrahydrofuran or N,N-dimethylformamide, at atemperature of from 0° to 100° C. (preferably 0° to 50° C.).

According to a further feature of the invention compounds of formula (I)wherein N=Q is a formula (A) which is a heterocyclic ring of formula(A¹) or (A⁴), m is zero, Y is S and the other symbols are as definedabove, may be prepared by the cyclisation reaction of a compound offormula (IX) or (X) respectively:

wherein the various symbols are as defined above and L₁ is a leavinggroup, generally halogen and preferably chlorine or bromine. Thereaction is generally performed in the presence of an organic base suchas a tertiary amine for example triethylamine, or pyridine, or aninorganic base such as an alkali metal carbonate, for example potassiumcarbonate, or an alkali metal alkoxide such as sodium ethoxide, orsodium hydride, in a solvent such as dioxan, tetrahydrofuran orN,N-dimethylformamide, at a temperature of from 0° to 100° C.(preferably 0° to 50° C.).

According to a further feature of the invention compounds of formula (I)wherein m is zero and N=Q is a formula (B) in which R¹ and R⁴ are asdefined above, may be prepared by the reaction of a compound of formula(XI):

wherein X, W and R⁴ are as defined above, with a compound of formula(III) as defined above. The reaction is generally performed in thepresence of an organic base such as a tertiary amine for exampletriethylamine, or pyridine, or an inorganic base such as an alkali metalcarbonate, for example potassium carbonate, or an alkali metal alkoxidesuch as sodium ethoxide, or sodium hydride, in a solvent such as dioxan,tetrahydrofuran or N,N-dimethylformamide, at a temperature of from 0° to100° C. (preferably 0° to 50° C.).

According to a further feature of the invention compounds of formula (I)wherein m is zero and N=Q is a formula (B) which is a heterocyclic ringof formula (B¹) or (B²), wherein the various symbols are as definedabove, may be prepared by the cyclisation reaction of the correspondingcompound of formula (XII) or (XIII):

wherein L is a leaving group generally halogen and preferably chlorineor bromine, and the other symbols are as defined above. The reaction maybe conducted according to the conditions used for the preparation ofcompounds of formula (I) wherein m is zero and N=Q is a formula (B) inwhich R¹ and R⁴ are as defined above, from a compound of formula (XI)and a compound of formula (III).

According to a further feature of the invention compounds of formula (I)wherein Q is as defined above, and m is 1 may be prepared by oxidising acorresponding compound in which m is 0. The oxidation is generallyperformed using hydrogen peroxide in a solvent such as acetic acid, or aperacid such as 3-chloroperbenzoic acid in a solvent such asdichloromethane or 1,2-dichloroethane, at a temperature of from 0° C. tothe reflux temperature of the solvent.

Compounds of formula (VII) may be prepared according to the abovedescribed procedure for the preparation of compounds of formula (I) fromcompounds of formula (II) and (III).

Intermediates of formula (II) wherein Y is O, may be prepared by thereaction of a compound of formula (IV) above, with oxalyl chloride, inan inert solvent such as dichloroethane at a temperature of from 0° to60° C., to give the corresponding acylisocyanate intermediate which isgenerally not isolated, and which is directly reacted with an amine offormula (XIV):HNR²R³  (XIV)wherein R² and R³ are as defined above. The reaction is generallyperformed in an inert solvent such as dichloroethane or tetrahydrofuranat a temperature of from 0° to 60° C.

Intermediates of formula (II), (IX) and (X) wherein Y is O or S may beprepared by the reaction of a compound of formula (XV):

wherein Y is O or S, with a corresponding compound of formula (XIV). Thereaction is generally performed in an inert solvent such asdichloroethane or tetrahydrofuran at a temperature of from 0° to 60° C.

Intermediates of formula (VI) wherein L is chlorine, may be preparedaccording to known procedures, for example by the reaction of thecorresponding carboxylic acid wherein L is replaced by OH, with asuitable halogenating agent, preferably oxalyl chloride, in a solventsuch as dichloroethane, optionally in the presence ofN;N-dimethylformamide, at a temperature of from 0° to 60° C.

Intermediate of formula (XV) wherein Y is S, may be prepared accordingto known procedures, for example by the reaction of a compound offormula (VI) as defined above, with an alkali metal thiocyanate orammonium thiocyanate or tetraalkylammonium thiocyanate for exampletetrabutylammonium thiocyanate, in the presence of a base such as analkali metal carbonate for example potassium carbonate, at a temperatureof from 0° to 60° C.

Intermediate of formula (XV) wherein Y is O, may be prepared accordingto known procedures, for example by the reaction of a compound offormula (VI) as defined above, with an alkali metal cyanate or ammoniumcyanate or tetraalkylammonium cyanate for example tetrabutylammoniumcyanate, in the presence of a base such as an alkali metal carbonate forexample potassium carbonate, at a temperature of from 0° to 60° C.

Intermediates of formula (XI), (XII) and (XIII) wherein Y is O or S maybe prepared by the reaction of a compound of formula (XV) as definedabove, with a corresponding compound of formula (XVI):HWR⁴  (XVI)wherein W and R⁴ are as defined above. The reaction is generallyperformed in an inert solvent such as dichloroethane or tetrahydrofuranat a temperature of from 0° to 60° C.

Collections of compounds of the formula (I) which can be synthesized bythe above mentioned process may also be prepared in a parallel manner,and this may be effected manually or in a semiautomated or fullyautomated manner. In this case, it is possible, for example, to automatethe procedure of the reaction, work-up or purification of the productsor of the intermediates. In total, this is to be understood as meaning aprocedure as is described, for example, by S. H. DeWitt in “AnnualReports in Combinatorial Chemistry and Molecular Diversity: AutomatedSynthesis”, Volume 1, Verlag Escom 1997, pages 69 to 77.

A series of commercially available apparatuses as are offered by, forexample, Stem Corporation, Woodrolfe Road, Tollesbury, Essex, CM9 8SE,England or H+P Labortechnik GmbH, Bruckmannring 28, 85764Oberschleiβheim, Germany or Radleys, Shirehill, Saffron Walden, Essex,England, may be used for the parallel procedure of the reaction andwork-up. For the parallel purification of compounds of the formula (I),or of intermediates obtained during the preparation, use may be made,inter alia, of chromatography apparatuses, for example those by ISCO,Inc., 4700 Superior Street, Lincoln, Nebr. 68504, USA.

The apparatuses mentioned lead to a modular procedure in which theindividual process steps are automated, but manual operations must beperformed between the process steps. This can be prevented by employingsemi-integrated or fully integrated automation systems where theautomation modules in question are operated by, for example, robots.Such automation systems can be obtained, for example, from ZymarkCorporation, Zymark Center, Hopkinton, Mass. 01748, USA.

In addition to what has been described here, compounds of the formula(I) may be prepared in part or fully by solid-phase-supported methods.For this purpose, individual intermediate steps or all intermediatesteps of the synthesis or of a synthesis adapted to suit the procedurein question are bound to a synthetic resin. Solid-phase-supportedsynthesis methods are described extensively in the specialistliterature, for example Barry A. Bunin in “The Combinatorial Index”,Academic Press, 1998.

The use of solid-phase-supported synthesis methods permits a series ofprotocols which are known from the literature and which, in turn, can beperformed manually or in an automated manner. For example, the “tea-bagmethod” (Houghten, U.S. Pat. No. 4,631,211; Houghten et al., Proc. Natl.Acad. Sci, 1985, 82, 5131-5135), in which products by IRORI, 11149 NorthTorrey Pines Road, La Jolla, Calif. 92037, USA, are employed, may besemiautomated. The automation of solid-phase-supported parallelsyntheses is performed successfully, for example, by apparatuses byArgonaut Technologies, Inc., 887 Industrial Road, San Carlos, Calif.94070, USA or MultiSyn Tech GmbH, Wullener Feld 4, 58454 Witten,Germany.

The preparation of the processes described herein yields compounds ofthe formula (I) in the form of substance collections which are termedlibraries. The present invention also relates to libraries whichcomprise at least two compounds of the formula (I).

Compounds of formula (III), (IV), (V), (VI), (VIII), (XIV), (XVI),(A^(1a)), (A^(2a)), (A^(3a)) and (A^(4a)) are known or may be preparedby known methods.

The following non-limiting Examples illustrate the preparation of thecompounds of formula (I).

CHEMICAL EXAMPLES

NMR spectra were run in deuterochloroform unless stated otherwise.

In the Examples which follow, quantities (also percentages) areweight-based, unless stated otherwise.

Example 1

Sodium hydride (0.09 g, 60% dispersion in mineral oil) was added to asolution of 4-trifluoromethyl-3-pyridinecarboxamide (0.40 g) inN,N-dimethylformamide at 20° C. and stirred for an hour. Benzylisothiocyanate (0.31 ml) was added to the mixture and stirred at 20° C.for 2 hours, then allyl bromide (0.30 ml) added with stirring at 20° C.for 5 hours. Ethyl acetate and water were added and the organic phasedried (magnesium sulfate), evaporated and purified by columnchromatography on silica gel eluting with n-hexane/ethyl acetate (3:1)to give1-benzyl-S-(2-propenyl)-3-(4-trifluoromethyl-3-pyridylcarbonyl)isothiourea(0.55 g, Compound A-724).

Example 2

Sodium hydride (0.03 g, 60% dispersion in mineral oil) was added to asolution of1-methyl-1-phenyl-3-(4-trifluoromethyl-3-pyridylcarbonyl)thiourea (0.2g) in tetrahydrofuran, and stirred at 20° C. for 1 hour. Allyl bromide(0.31 ml) was added and stirred at 20° C. for 2 hours, then a furtheramount of allyl bromide (0.09 ml) added and stirred for 2 hours. Ethylacetate and water were added, the organic phase dried (magnesiumsulfate), evaporated and the residue purified by column chromatographyon silica gel, eluting with n-hexane/ethyl acetate (3:1) to giveI-methyl-1-phenyl-S-(2-propenyl)-3-(4-trifluoromethyl-3-pyridylcarbonyl)isothiourea(0.17 g, Compound A-1325).

Example 3

Sodium hydride (0.09 g, 60% dispersion in mineral oil) was added to asolution of 4-trifluoromethyl-3-pyridinecarboxamide (0.40 g) inN,N-dimethylformamide at 20° C., and stirred for an hour. Benzylisothiocyanate (0.31 ml) was added to the mixture and stirred at 20° C.for 2 hours, then methyl bromoacetate (0.30 ml) added and stirred at 20°C. for 5 hours. Ethyl acetate and water were added, the organic phasedried (magnesium sulfate), evaporated and the residue purified by silicagel column chromatography eluting with n-hexane/ethyl acetate (3:1) togive3-benzyl-2-(4-trifluoromethyl-3-pyridylcarbonyl)imino-4-thiazolidone(0.50 g, Compound D-143):

Example 4

Sodium hydride (0.09 g, 60% dispersion in mineral oil) was addedportionwise to a solution of 4-trifluoromethyl-3-pyridinecarboxamide(0.40 g) in N,N-dimethylformamide at 20° C., and stirred for 1 hour.Benzyl isothiocyanate (0.31 ml) was added and stirred at 20° C. for 1hour, then 1,2-dibromoethane (0.30 ml) added and stirred at 20° C. for 1hour. Sodium hydride (0.09 g, 60% dispersion in mineral oil) was addedin portions to the solution then stirred for 5 hours. Ethyl acetate andwater were added, the organic phase dried (magnesium sulfate),evaporated and the residue purified by silica gel column chromatographyeluting with n-hexane/ethyl acetate (3:1) to give3-benzyl-2-(4-trifluoromethyl-3-pyridylcarbonyl)iminothiazolidine (0.50g, Compound D-40).

Example 5

Methanesulfonyl chloride (0.14 ml) was added to an ice-cooled solutionof1-(2-hydroxyethyl)-1-phenyl-3-(4-trifluoromethyl-3-pyridylcarbonyl)thiourea(0.60 g) and triethylamine (0.42 ml) in dichloromethane, and stirred for3 hours at 20° C. The mixture was washed (water), dried (magnesiumsulfate), evaporated and the residue recrystallized (ethanol) to give3-phenyl-2-(4-trifluoromethyl-3-pyridylcarbonyl)iminothiazolidine (0.26g, Compound D-60).

Example 6

Oxalyl chloride (0.6 ml) was added to a suspension of4-trifluoromethylnicotinic acid (1 g) and a catalytic amount ofN,N-dimethylformamide in dichloromethane, and stirred at 20° C. for 1hour. 4-Benzyl-5-imino-1,3,4-thiadiazoline hydrobromide (1.44 g) wasadded under ice cooling, and was stirred at 20° C. for 1 hour. Themixture was then washed (water), dried (magnesium sulfate), evaporatedand the residue recrystallized (ethanol) to give4-benzyl-5-(4-trifluoromethyl-3-pyridylcarbonyl)imino-1,3,4-thiadiazoline(0.3 g, Compound E-39).

Example 7

Methanesulfonyl chloride (0.12 ml) was added to an ice-cooled solutionof1-(2-hydroxymethylphenyl)-3-(4-trifluoromethyl-3-pyridylcarbonyl)thiourea(0.50 g) and triethylamine (0.24 ml) in dichloromethane, and stirred for3 hours at 20° C. The reaction mixture was washed (water), dried(magnesium sulfate), evaporated and the residue recrystallized (ethanol)to give2-(4-trifluoromethyl-3-pyridylcarbonyl)imino-4,5-benzo-1,3-thiazine (0.1g, Compound G-1).

The following Reference Example illustrates the preparation ofintermediates used in the synthesis of the above Examples.

Reference Example 1

Oxalyl chloride (3.2 ml, 2M) was added to a suspension4-trifluoromethylnicotinic acid (1 g) and a catalytic amount ofN,N-dimethylformamide in dichloromethane, and stirred at 20° C. for 1hour. The mixture was evaporated, the residue dissolved in toluene andtetrabutylammonium thiocyanate (1 g) and potassium carbonate (0.5 g)added, then stirred at 20° C. for 30 minutes to give4-trifluoromethyl-3-pyridylcarbonyl isothiocyanate. 2-Anilinoethanol(1.86 g) was then added, and the mixture stirred at 20° C. for 1 hour.Ethyl acetate was added and the mixture washed with water, hydrochloricacid 1(M), saturated sodium bicarbonate and brine, dried (magnesiumsulfate), evaporated and recrystallised from ethanol to give1-(2′-hydroxyethyl)-1-phenyl-3-(4-trifluoromethyl-3-pyridylcarbonyl)thiourea(0.9 g); NMR 3.95(2H, t), 4.38(2H, m), 7.3-7.6(6H, m), 8.50(1H, brs),8.80(1H, d).

By proceeding in a similar manner the following intermediates were alsoprepared:

-   1-methyl-1-phenyl-3-(4-trifluoromethyl-3-pyridylcarbonyl)thiourea,    NMR 3.69(1H, s), 7.3-7.6(6H, m), 8.33(1H, brs), 8.51(1H, s), 8.79(1    h, d); and-   1-(2-hydroxymethylphenyl)-3-(4-trifluoromethyl-3-pyridylcarbonyl)thiourea,    NMR 4.71(2H, s), 7.2-7.4(2H, m), 7.5-7.6(1H, m), 7.8-7.9(2H, m),    9.01(1H, d), 9.11(1H, s), 11.01(1H, brs), 12.13(1H, brs).

The following preferred compounds shown in Tables 1 to 9 also form partof the present invention, and were or may be prepared in accordancewith, or analogously to, the above-mentioned Examples 1 to 7 or theabove-described general methods. In the Tables Ph means phenyl and Memeans methyl. Where subscripts are omitted after atoms it will beunderstood that they are intended, for example CH3 means CH₃.

Compound numbers are given for reference purposes only.

TABLE I Compounds of formula (Ia): (Ia)

Compound R¹ R² R A-1 CH3 CH3 H A-2 C2H5 CH3 H A-3 n-C3H7 CH3 H A-4i-C3H7 CH3 H A-5 n-C4H9 CH3 H A-6 s-C4H9 CH3 H A-7 i-C4H9 CH3 H A-8t-C4H9 CH3 H A-9 n-C5H11 CH3 H A-10 n-C6H13 CH3 H A-11 CH2CH═CH2 CH3 HA-12 CH2C(CH3)═CH2 CH3 H A-13 CH2C(CH3)═CHCH3 CH3 H A-14 CH2CH═C(CH3)2CH3 H A-15 CH2CCl═CH2 CH3 H A-16 CH2CH═CCl2 CH3 H A-17 CH2CH═CHCF3 CH3 HA-18 CH2CH═CHPh CH3 H A-19 CH(CH3)CH═CH2 CH3 H A-20 CH2CCH CH3 H A-21CH2CCCH3 CH3 H A-22 CH2CF3 CH3 H A-23 CH2CH2OCH3 CH3 H A-24 CH2CH2OC2H5CH3 H A-25 CH2CH2OH2OCH3 CH3 H A-26 CH2CH2CH2OC2H5 CH3 H A-27CH2CH(OCH3)2 CH3 H A-28 CH2CN CH3 H A-29 CH2(cyclo-C3H5) CH3 H A-30CH2(cyclo-C5H9) CH3 H A-31 CH2(cyclo-C6H11) CH3 H A-32 CH2Ph CH3 H A-33CH2(2-Cl-Ph) CH3 H A-34 CH2(3-Cl-Ph) CH3 H A-35 CH2(4-Cl-Ph) CH3 H A-36CH2(2-CF3-Ph) CH3 H A-37 CH2(3-CF3-Ph) CH3 H A-38 CH2(4-CF3-Ph) CH3 HA-39 CH2(2-F-Ph) CH3 H A-40 CH2(3-F-Ph) CH3 H A-41 CH2(4-F-Ph) CH3 HA-42 CH2(2-OMe-Ph) CH3 H A-43 CH2(3-OMe-Ph) CH3 H A-44 CH2(4-OMe-Ph) CH3H A-45 CH(CH3)Ph CH3 H A-46 CH(CH3)(2-Cl-Ph) CH3 H A-47 CH(CH3)(3-Cl-Ph)CH3 H A-48 CH(CH3)(4-Cl-Ph) CH3 H A-49 CH(CH3)(2-CF3-Ph) CH3 H A-50CH(CH3)(3-CF3-Ph) CH3 H A-51 CH(CH3)(4-CF3-Ph) CH3 H A-52 CH2CH2Ph CH3 HA-53 CH3 CH3 CH3 A-54 C2H5 CH3 CH3 A-55 n-C3H7 CH3 CH3 A-56 i-C3H7 CH3CH3 A-57 n-C4H9 CH3 CH3 A-58 s-C4H9 CH3 CH3 A-59 i-C4H9 CH3 CH3 A-60t-C4H9 CH3 CH3 A-61 n-C5H11 CH3 CH3 A-62 n-C6H13 CH3 CH3 A-63 CH2CH═CH2CH3 CH3 A-64 CH2C(CH3)═CH2 CH3 CH3 A-65 CH2C(CH3)═CHCH3 CH3 CH3 A-66CH2CH═C(CH3)2 CH3 CH3 A-67 CH2CCl═CH2 CH3 CH3 A-68 CH2CH═CCl2 CH3 CH3A-69 CH2CH═CHCF3 CH3 CH3 A-70 CH2CH═CHPh CH3 CH3 A-71 CH(CH3)CH═CH2 CH3CH3 A-72 CH2CCH CH3 CH3 A-73 CH2CCCH3 CH3 CH3 A-74 CH2CF3 CH3 CH3 A-75CH2CH2OCH3 CH3 CH3 A-76 CH2CH2OC2H5 CH3 CH3 A-77 CH2CH2CH2OCH3 CH3 CH3A-78 CH2CH2CH2OC2H5 CH3 CH3 A-79 CH2CH(OCH3)2 CH3 CH3 A-80 CH2CN CH3 CH3A-81 CH2(cyclo-C3H5) CH3 CH3 A-82 CH2(cyclo-C5H9) CH3 CH3 A-83CH2(cyclo-C6H11) CH3 CH3 A-84 CH2CO2CH3 CH3 CH3 A-85 CH2CO2C2H5 CH3 CH3A-86 CH(CH3)CO2CH3 CH3 CH3 A-87 CH(CH3)CO2C2H5 CH3 CH3 A-88C(CH3)2CO2CH3 CH3 CH3 A-89 CH2Ph CH3 CH3 A-90 CH2(2-Cl-Ph) CH3 CH3 A-91CH2(3-Cl-Ph) CH3 CH3 A-92 CH2(4-Cl-Ph) CH3 CH3 A-93 CH2(2-CF3-Ph) CH3CH3 A-94 CH2(3-CF3-Ph) CH3 CH3 A-95 CH2(4-CF3-Ph) CH3 CH3 A-96CH2(2-F-Ph) CH3 CH3 A-97 CH2(3-F-Ph) CH3 CH3 A-98 CH2(4-F-Ph) CH3 CH3A-99 CH2(2-OMe-Ph) CH3 CH3 A-100 CH2(3-OMe-Ph) CH3 CH3 A-101CH2(4-OMe-Ph) CH3 CH3 A-102 CH(CH3)Ph CH3 CH3 A-103 CH(CH3)(2-Cl-Ph) CH3CH3 A-104 CH(CH3)(3-Cl-Ph) CH3 CH3 A-105 CH(CH3)(4-Cl-Ph) CH3 CH3 A-106CH(CH3)(2-CF3-Ph) CH3 CH3 A-107 CH(CH3)(3-CF3-Ph) CH3 CH3 A-108CH(CH3)(4-CF3-Ph) CH3 CH3 A-109 CH2CH2Ph CH3 CH3 A-110 CH3 C2H5 H A-111C2H5 C2H5 H A-112 n-C3H7 C2H5 H A-113 i-C3H7 C2H5 H A-114 n-C4H9 C2H5 HA-115 s-C4H9 C2H5 H A-116 i-C4H9 C2H5 H A-117 t-C4H9 C2H5 H A-118n-C5H11 C2H5 H A-119 n-C6H13 C2H5 H A-120 CH2CH═CH2 C2H5 H A-121CH2C(CH3)═CH2 C2H5 H A-122 CH2C(CH3)═CHCH3 C2H5 H A-123 CH2CH═C(CH3)2C2H5 H A-124 CH2CCl═CH2 C2H5 H A-125 CH2CH═CCl2 C2H5 H A-126 CH2CH═CHCF3C2H5 H A-127 CH2CH═CHPh C2H5 H A-128 CH(CH3)CH═CH2 C2H5 H A-129 CH2CCHC2H5 H A-130 CH2CCCH3 C2H5 H A-131 CH2CF3 C2H5 H A-132 CH2CH2OCH3 C2H5 HA-133 CH2CH2OC2H5 C2H5 H A-134 CH2CH2CH2OCH3 C2H5 H A-135 CH2CH2CH2OC2H5C2H5 H A-136 CH2CH(OCH3)2 C2H5 H A-137 CH2CN C2H5 H A-138CH2(cyclo-C3H5) C2H5 H A-139 CH2(cyclo-C5H9) C2H5 H A-140CH2(cyclo-C6H11) C2H5 H A-141 CH2Ph C2H5 H A-142 CH2(2-Cl-Ph) C2H5 HA-143 CH2(3-Cl-Ph) C2H5 H A-144 CH2(4-Cl-Ph) C2H5 H A-145 CH2(2-CF3-Ph)C2H5 H A-146 CH2(3-CF3-Ph) C2H5 H A-147 CH2(4-CF3-Ph) C2H5 H A-148CH2(2-F-Ph) C2H5 H A-149 CH2(3-F-Ph) C2H5 H A-150 CH2(4-F-Ph) C2H5 HA-151 CH2(2-OMe-Ph) C2H5 H A-152 CH2(3-OMe-Ph) C2H5 H A-153CH2(4-OMe-Ph) C2H5 H A-154 CH(CH3)Ph C2H5 H A-155 CH(CH3)(2-Cl-Ph) C2H5H A-156 CH(CH3)(3-Cl-Ph) C2H5 H A-157 CH(CH3)(4-Cl-Ph) C2H5 H A-158CH(CH3)(2-CF3-Ph) C2H5 H A-159 CH(CH3)(3-CF3-Ph) C2H5 H A-160CH(CH3)(4-CF3-Ph) C2H5 H A-161 CH2CH2Ph C2H5 H A-162 CH3 C2H5 C2H5 A-163C2H5 C2H5 C2H5 A-164 n-C3H7 C2H5 C2H5 A-165 i-C3H7 C2H5 C2H5 A-166n-C4H9 C2H5 C2H5 A-167 s-C4H9 C2H5 C2H5 A-168 i-C4H9 C2H5 C2H5 A-169t-C4H9 C2H5 C2H5 A-170 n-C5H11 C2H5 C2H5 A-171 n-C6H13 C2H5 C2H5 A-172CH2CH═CH2 C2H5 C2H5 A-173 CH2C(CH3)═CH2 C2H5 C2H5 A-174 CH2C(CH3)═CHCH3C2H5 C2H5 A-175 CH2CH═C(CH3)2 C2H5 C2H5 A-176 CH2CC═CH2 C2H5 C2H5 A-177CH2CH═CCl2 C2H5 C2H5 A-178 CH2CH═CHCF3 C2H5 C2H5 A-179 CH2CH═CHPh C2H5C2H5 A-180 CH(CH3)CH═CH2 C2H5 C2H5 A-181 CH2CCH C2H5 C2H5 A-182 CH2CCCH3C2H5 C2H5 A-183 CH2CF3 C2H5 C2H5 A-184 CH2CH2OCH3 C2H5 C2H5 A-185CH2CH2OC2H5 C2H5 C2H5 A-186 CH2CH2CH2OCH3 C2H5 C2H5 A-187 CH2CH2CH2OC2H5C2H5 C2H5 A-188 CH2CH(OCH3)2 C2H5 C2H5 A-189 CH2CN C2H5 C2H5 A-190CH2(cyclo-C3H5) C2H5 C2H5 A-191 CH2(cyclo-C5H9) C2H5 C2H5 A-192CH2(cyclo-C6H11) C2H5 C2H5 A-193 CH2OC2CH3 C2H5 C2H5 A-194 CH2CO2C2H5C2H5 C2H5 A-195 CH(CH3)CO2CH3 C2H5 C2H5 A-196 CH(CH3)CO2C2H5 C2H5 C2H5A-197 C(CH3)2CO2CH3 C2H5 C2H5 A-198 CH2Ph C2H5 C2H5 A-199 CH2(2-Cl-Ph)C2H5 C2H5 A-200 CH2(3-Cl-Ph) C2H5 C2H5 A-201 CH2(4-Cl-Ph) C2H5 C2H5A-202 CH2(2-CF3-Ph) C2H5 C2H5 A-203 CH2(3-CF3-Ph) C2H5 C2H5 A-204CH2(4-CF3-Ph) C2H5 C2H5 A-205 CH2(2-F-Ph) C2H5 C2H5 A-2C6 CH2(3-F-Ph)C2H5 C2H5 A-207 CH2(4-F-Ph) C2H5 C2H5 A-208 CH2(2-OMe-Ph) C2H5 C2H5A-209 CH2(3-OMe-Ph) C2H5 C2H5 A-210 CH2(4-OMe-Ph) C2H5 C2H5 A-211CH(CH3)Ph C2H5 C2H5 A-212 CH(CH3)(2-Cl-Ph) C2H5 C2H5 A-213CH(CH3)(3-Cl-Ph) C2H5 C2H5 A-214 CH(CH3)(4-Cl-Ph) C2H5 C2H5 A-215CH(CH3)(2-CF3-Ph) C2H5 C2H5 A-216 CH(CH3)(3-CF3-Ph) C2H5 C2H5 A-217CH(CH3)(4-CF3-Ph) C2H5 C2H5 A-218 CH2CH2Ph C2H5 C2H5 A-219 CH3 i-C3H7 HA-220 C2H5 i-C3H7 H A-221 n-C3H7 i-C3H7 H A-222 i-C3H7 i-C3H7 H A-223n-C4H9 i-C3H7 H A-224 s-C4H9 i-C3H7 H A-225 i-C4H9 i-C3H7 H A-226 t-C4H9i-C3H7 H A-227 n-C5H11 i-C3H7 H A-228 n-C6H13 i-C3H7 H A-229 CH2CH═CH2i-C3H7 H A-230 CH2C(CH3)═CH2 i-C3H7 H A-231 CH2CH═CHCH3 i-C3H7 H A-232CH2CH═C(CH3)2 i-C3H7 H A-233 CH2CCl═CH2 i-C3H7 H A-234 CH2CH═CCl2 i-C3H7H A-235 CH2CH═CHCF3 i-C3H7 H A-236 CH2CH═CHPh i-C3H7 H A-237CH(CH3)CH═CH2 i-C3H7 H A-238 CH2CCH i-C3H7 H A-239 CH2CCCH3 i-C3H7 HA-240 CH2CF3 i-C3H7 H A-241 CH2CH2OCH3 i-C3H7 H A-242 CH2CH2OC2H5 i-C3H7H A-243 CH2CH2CH2OCH3 i-C3H7 H A-244 CH2CH2CH2OC2H5 i-C3H7 H A-245CH2CH(OCH3)2 i-C3H7 H A-246 CH2CN i-C3H7 H A-247 CH2(cyclo-C3H5) i-C3H7H A-248 CH2(cyclo-C5H9) i-C3H7 H A-249 CH2(cyclo-C6H11) i-C3H7 H A-250CH2Ph i-C3H7 H A-251 CH2(2-Cl-Ph) i-C3H7 H A-252 CH2(3-Cl-Ph) i-C3H7 HA-253 CH2(4-Cl-Ph) i-C3H7 H A-254 CH2(2-CF3-Ph) i-C3H7 H A-255CH2(3-CF3-Ph) i-C3H7 H A-256 CH2(4-CF3-Ph) i-C3H7 H A-257 CH2(2-F-Ph)i-C3H7 H A-258 CH2(3-F-Ph) i-C3H7 H A-259 CH2(4-F-Ph) i-C3H7 H A-260CH2(2-OMe-Ph) i-C3H7 H A-261 CH2(3-OMe-Ph) i-C3H7 H A-262 CH2(4-OMe-Ph)i-C3H7 H A-263 CH(CH3)Ph i-C3H7 H A-264 CH(CH3)(2-Cl-Ph) i-C3H7 H A-265CH(CH3)(3-Cl-Ph) i-C3H7 H A-266 CH(CH3)(4-Cl-Ph) i-C3H7 H A-267CH(CH3)(2-CF3-Ph) i-C3H7 H A-268 CH(CH3)(3-CF3-Ph) i-C3H7 H A-269CH(CH3)(4-CF3-Ph) i-C3H7 H A-270 CH2CH2Ph i-C3H7 H A-271 CH3 n-C3H7 HA-272 C2H5 n-C3H7 H A-273 n-C3H7 n-C3H7 H A-274 i-C3H7 n-C3H7 H A-275n-C4H9 n-C3H7 H A-276 s-C4H9 n-C3H7 H A-277 i-C4H9 n-C3H7 H A-278 t-C4H9n-C3H7 H A-279 n-C5H11 n-C3H7 H A-280 n-C6H13 n-C3H7 H A-281 CH2CH═CH2n-C3H7 H A-282 CH2C(CH3)═CH2 n-C3H7 H A-283 CH2CH═CHCH3 n-C3H7 H A-284CH2CH═C(CH3)2 n-C3H7 H A-285 CH2CCl═CH2 n-C3H7 H A-286 CH2CH═CCl2 n-C3H7H A-287 CH2CH═CHCF3 n-C3H7 H A-288 CH2CH═CHPh n-C3H7 H A-289CH(CH3)CH═CH2 n-C3H7 H A-290 CH2CCH n-C3H7 H A-291 CH2CCCH3 n-C3H7 HA-292 CH2CF3 n-C3H7 H A-293 CH2CH2OCH3 n˜C3H7 H A-294 CH2CH2OC2H5 n-C3H7H A-295 CH2CH2CH2OCH3 n-C3H7 H A-296 CH2CH2CH2OC2H5 n-C3H7 H A-297CH2CH(OCH3)2 n-C3H7 H A-298 CH2CN n-C3H7 H A-299 CH2(cyclo-C3H5) n-C3H7H A-300 CH2(cyclo-C5H9) n-C3H7 H A-301 CH2(cyclo-C6H11) n-C3H7 H A-302CH2Ph n-C3H7 H A-303 CH2(2-Cl-Ph) n-C3H7 H A-304 CH2(3-Cl-Ph) n-C3H7 HA-305 CH2(4-Cl-Ph) n-C3H7 H A-3C6 CH2(2-CF3-Ph) n-C3H7 H A-307CH2(3-CF3-Ph) n-C3H7 H A-308 CH2(4-CF3-Ph) n-C3H7 H A-309 CH2(2-F-Ph)n-C3H7 H A-310 CH2(3-F-Ph) n-C3H7 H A-311 CH2(4-F-Ph) n-C3H7 H A-312CH2(2-OMe-Ph) n-C3H7 H A-313 CH2(3-OMe-Ph) n-C3H7 H A-314 CH2(4-OMe-Ph)n-C3H7 H A-315 CH(CH3)Ph n-C3H7 H A-316 CH(CH3)(2-Cl-Ph) n-C3H7 H A-317CH(CH3)(3-Cl-Ph) n-C3H7 H A-318 CH(CH3)(4-Cl-Ph) n-C3H7 H A-319CH(CH3)(2-CF3-Ph) n-C3H7 H A-320 CH(CH3)(3-CF3-Ph) n-C3H7 H A-321CH(CH3)(4-CF3-Ph) n-C3H7 H A-322 CH2CH2Ph n-C3H7 H A-323 CH3 n-C4H9 HA-324 C2H5 n-C4H9 H A-325 n-C3H7 n-C4H9 H A-328 i-C3H7 n-C4H9 H A-327n-C4H9 n-C4H9 H A-328 s-C4H9 n-C4H9 H A-329 i-C4H9 n-C4H9 H A-330 t-C4H9n-C4H9 H A-331 n-C5H11 n-C4H9 H A-332 n-C6H13 n-C4H9 H A-333 CH2CH═CH2n-C4H9 H A-334 CH2C(CH3)═CH2 n-C4H9 H A-335 CH2C(CH3)═CHCH3 n-C4H9 HA-336 CH2CH═C(CH3)2 n-C4H9 H A-337 CH2CCl═CH2 n-C4H9 H A-338 CH2CH═CCl2n-C4H9 H A-339 CH2CH═CHCF3 n-C4H9 H A-340 CH2CH═CHPh n-C4H9 H A-341CH(CH3)CH═CH2 n-C4H9 H A-342 CH2CCH n-C4H9 H A-343 CH2CCCH3 n-C4H9 HA-344 CH2CF3 n-C4H9 H A-345 CH2CH2OCH3 n-C4H9 H A-346 CH2CH2OC2H5 n-C4H9H A-347 CH2CH2CH2OCH3 n-C4H9 H A-348 CH2CH2CH2OC2H5 n-C4H9 H A-349CH2CH(OCH3)2 n-C4H9 H A-350 CH2CN n-C4H9 H A-351 CH2(cyclo-C3H5) n-C4H9H A-352 CH2(cyclo-C5H9) n-C4H9 H A-353 CH2(cyclo-C6H11) n-C4H9 H A-354CH2Ph n-C4H9 H A-355 CH2(2-Cl-Ph) n-C4H9 H A-356 CH2(3-Cl-Ph) n-C4H9 HA-357 CH2(4-Cl-Ph) n-C4H9 H A-358 CH2(2-CF3-Ph) n-C4H9 H A-359CH2(3-CF3-Ph) n-C4H9 H A-360 CH2(4-CF3-Ph) n-C4H9 H A-361 CH2(2-F-Ph)n-C4H9 H A-362 CH2(3-F-Ph) n-C4H9 H A-363 CH2(4-F-Ph) n-C4H9 H A-364CH2(2-OMe-Ph) n-C4H9 H A-365 CH2(3-OMe-Ph) n-C4H9 H A-366 CH2(4-OMe-Ph)n-C4H9 H A-367 CH(CH3)Ph n-C4H9 H A-368 CH(CH3)(2-Cl-Ph) n-C4H9 H A-369CH(CH3)(3-Cl-Ph) n-C4H9 H A-370 CH(CH3)(4-Cl-Ph) n-C4H9 H A-371CH(CH3)(2-CF3-Ph) n-C4H9 H A-372 CH(CH3)(3-CF3-Ph) n-C4H9 H A-373CH(CH3)(4-CF3-Ph) n-C4H9 H A-374 CH2CH2Ph n-C4H9 H A-375 CH3 s-C4H9 HA-376 C2H5 s-C4H9 H A-377 n-C3H7 s-C4H9 H A-378 i-C3H7 s-C4H9 H A-379n-C4H9 s-C4H9 H A-380 s-C4H9 s-C4H9 H A-381 i-C4H9 s-C4H9 H A-382 t-C4H9s-C4H9 H A-383 n-C5H11 s-C4H9 H A-384 n-C6H13 s-C4H9 H A-385 CH2CH═CH2s-C4H9 H A-386 CH2C(CH3)═CH2 s-C4H9 H A-387 CH2CH═CHCH3 s-C4H9 H A-388CH2CH═C(CH3)2 s-C4H9 H A-389 CH2CCl═CH2 s-C4H9 H A-390 CH2CH═CCl2 s-C4H9H A-391 CH2CH═CHCF3 s-C4H9 H A-392 CH2CH═CHPh s-C4H9 H A-393CH(CH3)CH═CH2 s-C4H9 H A-394 CH2CCH s-C4H9 H A-395 CH2CCCH3 s-C4H9 HA-395 CH2CF3 s-C4H9 H A-397 CH2CH2OCH3 s-C4H9 H A-398 CH2CH2OC2H5 s-C4H9H A-399 CH2CH2CH2OCH3 s-C4H9 H A-400 CH2CH2CH2OC2H5 s-C4H9 H A-401CH2CH(OCH3)2 s-C4H9 H A-402 CH2CN s-C4H9 H A-403 CH2(cyclo-C3H5) s-C4H9H A-404 CH2(cyclo-C5H9) s-C4H9 H A-405 CH2(cyclo-C6H11) s-C4H9 H A-406CH2Ph s-C4H9 H A-407 CH2(2-Cl-Ph) s-C4H9 H A-408 CH2(3-Cl-Ph) s-C4H9 HA-409 CH2(4-Cl-Ph) s-C4H9 H A-410 CH2(2-CF3-Ph) s-C4H9 H A-411CH2(3-CF3-Ph) s-C4H9 H A-412 CH2(4-CF3-Ph) s-C4H9 H A-413 CH2(2-F-Ph)s-C4H9 H A-414 CH2(3-F-Ph) s-C4H9 H A-415 CH2(4-F-Ph) s-C4H9 H A-416CH2(2-OMe-Ph) s-C4H9 H A-417 CH2(3-OMe-Ph) s-C4H9 H A-418 CH2(4-OMe-Ph)s-C4H9 H A-419 CH(CH3)Ph s-C4H9 H A-420 CH(CH3)(2-Cl-Ph) s-C4H9 H A-421CH(CH3)(3-Cl-Ph) s-C4H9 H A-422 CH(CH3)(4-Cl-Ph) s-C4H9 H A-423CH(CH3)(2-CF3-Ph) s-C4H9 H A-424 CH(CH3)(3-CF3-Ph) s-C4H9 H A-425CH(CH3)(4-CF3-Ph) s-C4H9 H A-426 CH2CH2Ph s-C4H9 H A-427 CH3 i-C4H9 HA-428 C2H5 i-C4H9 H A-429 n-C3H7 i-C4H9 H A-430 i-C3H7 i-C4H9 H A-431n-C4H9 i-C4H9 H A-432 s-C4H9 i-C4H9 H A-433 i-C4H9 i-C4H9 H A-434 t-C4H9i-C4H9 H A-435 n-C5H11 i-C4H9 H A-436 n-C6H13 i-C4H9 H A-437 CH2CH═CH2i-C4H9 H A-438 CH2C(CH3)═CH2 i-C4H9 H A-439 CH2CH═CHCH3 i-C4H9 H A-440CH2CH═C(CH3)2 i-C4H9 H A-441 CH2CCl═CH2 i-C4H9 H A-442 CH2CH═CCl2 i-C4H9H A-443 CH2CH═CHCF3 i-C4H9 H A-444 CH2CH═CHPh i-C4H9 H A-445CH(CH3)CH═CH2 i-C4H9 H A-446 CH2CCH i-C4H9 H A-447 CH2CCCH3 i-C4H9 HA-448 CH2CF3 i-C4H9 H A-449 CH2CH2OCH3 i-C4H9 H A-450 CH2CH2OC2H5 i-C4H9H A-451 CH2CH2CH2OCH3 i-C4H9 H A-452 CH2CH2CH2OC2H5 i-C4H9 H A-453CH2OH(OCH3)2 i-C4H9 H A-454 CH2CN i-C4H9 H A-455 CH2(cyclo-C3H5) i-C4H9H A-456 CH2(cyclo-C5H9) i-C4H9 H A-457 CH2(cyclo-C6H11) i-C4H9 H A-458CH2Ph i-C4H9 H A-459 CH2(2-Cl-Ph) i-C4H9 H A-460 CH2(3-Cl-Ph) i-C4H9 HA-461 CH2(4-Cl-Ph) i-C4H9 H A-462 CH2(2-CF3-Ph) i-C4H9 H A-463CH2(3-CF3-Ph) i-C4H9 H A-464 CH2(4-CF3-Ph) i-C4H9 H A-465 CH2(2-F-Ph)i-C4H9 H A-466 CH2(3-F-Ph) i-C4H9 H A-467 CH2(4-F-Ph) i-C4H9 H A-468CH2(2-OMe-Ph) i-C4H9 H A-469 CH2(3-OMe-Ph) i-C4H9 H A-470 CH2(4-OMe-Ph)i-C4H9 H A-471 CH(CH3)Ph i-C4H9 H A-472 CH(CH3)(2-Cl-Ph) i-C4H9 H A-473CH(CH3)(3-Cl-Ph) i-C4H9 H A-474 CH(CH3)(4-Cl-Ph) i-C4H9 H A-475CH(CH3)(2-CF3-Ph) i-C4H9 H A-476 CH(CH3)(3-CF3-Ph) i-C4H9 H A-477CH(CH3)(4-CF3-Ph) i-C4H9 H A-478 CH2CH2Ph i-C4H9 H A-479 CH3 t-C4H9 HA-480 C2H5 t-C4H9 H A-481 n-C3H7 t-C4H9 H A-482 i-C3H7 t-C4H9 H A-483n-C4H9 t-C4H9 H A-484 s-C4H9 t-C4H9 H A-485 i-C4H9 t-C4H9 H A-486 t-C4H9t-C4H9 H A-487 n-C5H11 t-C4H9 H A-488 n-C6H13 t-C4H9 H A-489 CH2CH═CH2t-C4H9 H A-490 CH2C(CH3)═CH2 t-C4H9 H A-491 CH2CH═CHCH3 t-C4H9 H A-492CH2CH═C(CH3)2 t-C4H9 H A-493 CH2CCl═CH2 t-C4H9 H A-494 CH2CH═CCl2 t-C4H9H A-495 CH2CH═CHCF3 t-C4H9 H A-496 CH2CH═CHPh t-C4H9 H A-497CH(CH3)CH═CH2 t-C4H9 H A-498 CH2CCH t-C4H9 H A-499 CH2CCCH3 t-C4H9 HA-500 CH2CF3 t-C4H9 H A-501 CH2CH2OCH3 t-C4H9 H A-502 CH2CH2OC2H5 t-C4H9H A-503 CH2CH2CH2OCH3 t-C4H9 H A-504 CH2OC2CH3 t-C4H9 H A-505CH2CH(OCH3)2 t-C4H9 H A-5C6 CH2CN t-C4H9 H A-507 CH2(cyclo-C3H5) t-C4H9H A-508 CH2(cyclo-C5H9) t-C4H9 H A-509 CH2(cyclo-C6H11) t-C4H9 H A-510CH2Ph t-C4H9 H A-511 CH2(2-Cl-Ph) t-C4H9 H A-512 CH2(3-Cl-Ph) t-C4H9 HA-513 CH2(4-Cl-Ph) t-C4H9 H A-514 CH2(2-CF3-Ph) t-C4H9 H A-515CH2(3-CF3-Ph) t-C4H9 H A-516 CH2(4-CF3-Ph) t-C4H9 H A-517 CH2(2-F-Ph)t-C4H9 H A-518 CH2(3-F-Ph) t-C4H9 H A-519 CH2(4-F-Ph) t-C4H9 H A-520CH2(2-OMe-Ph) t-C4H9 H A-521 CH2(3-OMe-Ph) t-C4H9 H A-522 CH2(4-OMe-Ph)t-C4H9 H A-523 CH(CH3)Ph t-C4H9 H A-524 CH(CH3)(2-Cl-Ph) t-C4H9 H A-525CH(CH3)(3-Cl-Ph) t-C4H9 H A-526 CH(CH3)(4-Cl-Ph) t-C4H9 H A-527CH(CH3)(2-CF3-Ph) t-C4H9 H A-528 CH(CH3)(3-CF3-Ph) t-C4H9 H A-529CH(CH3)(4-CF3-Ph) t-C4H9 H A-530 CH2CH2Ph t-C4H9 H A-531 n-C3H7 n-C5H11H A-532 i-C3H7 n-C5H11 H A-533 CH2CH═CH n-C5H11 H A-534 CH2C(CH3)═CH2n-C5H11 H A-535 CH2C(CH3)═CHCH3 n-C5H11 H A-536 CH2CH═C(CH3)2 n-C5H11 HA-537 CH2Ph n-C5H11 H A-538 CH2(3-CF3-Ph) n-C5H11 H A-539 n-C3H7C(CH3)2C2H5 H A-540 i-C3H7 C(CH3)2C2H5 H A-541 CH2CH═CH2 C(CH3)2C2H5 HA-542 CH2C(CH3)═CH2 C(CH3)2C2H5 H A-543 CH2C(CH3)═CHCH3 C(CH3)2C2H5 HA-544 CH2CH═C(CH3)2 C(CH3)2C2H5 H A-545 CH2Ph C(CH3)2C2H5 H A-546CH2(3-CF3-Ph) C(CH3)2C2H5 H A-547 n-C3H7 CH2CH2CH(CH3)CH3 H A-548 i-C3H7CH2CH2CH(CH3)CH3 H A-549 CH2CH═CH2 CH2CH2CH(CH3)CH3 H A-550CH2O(CH3)═CH2 CH2CH2CH(CH3)CH3 H A-551 CH2C(CH3)═CHCH3 CH2CH2CH(CH3)CH3H A-552 CH2CH═C(CH3)2 CH2CH2CH(CH3)CH3 H A-553 CH2Ph CH2CH2CH(CH3)CH3 HA-554 CH2(3-CF3-Ph) CH2CH2CH(CH3)CH3 H A-555 n-C3H7 CH2CH(CH3)C2H5 HA-556 i-C3H7 CH2CH(CH3)C2H5 H A-557 CH2CH═CH2 CH2CH(CH3)C2H5 H A-558CH2C(CH3)═CH2 CH2CH(CH3)C2H5 H A-559 CH2C(CH3)═CHCH3 CH2CH(CH3)C2H5 HA-560 CH2CH═C(CH3)2 CH2CH(CH3)C2H5 H A-561 CH2Ph CH2CH(CH3)C2H5 H A-562CH2(3-CF3-Ph) CH2CH(CH3)C2H5 H A-563 n-C3H7 n-C3H7 CH3 A-564 i-C3H7n-C3H7 CH3 A-565 CH2CH═CH n-C3H7 CH3 A-566 CH2C(CH3)═CH2 n-C3H7 CH3A-567 CH2C(CH3)═CHCH3 n-C3H7 CH3 A-568 CH2CH═C(CH3)2 n-C3H7 CH3 A-569CH2OC2CH3 n-C3H7 CH3 A-570 CH(CH3)CO2CH3 n-C3H7 CH3 A-571 C(CH3)2OC2CH3n-C3H7 CH3 A-572 CH2Ph n-C3H7 CH3 A-573 CH2(3-CF3-Ph) n-C3H7 CH3 A-574n-C3H7 n-C3H7 C2H5 A-575 i-C3H7 n-C3H7 C2H5 A-576 CH2CH═CH2 n-C3H7 C2H5A-577 CH2C(CH3)═CH2 n-C3H7 C2H5 A-578 CH2C(CH3)═CHCH3 n-C3H7 C2H5 A-579CH2CH═C(CH3)2 n-C3H7 C2H5 A-580 CH2CO2CH3 n-C3H7 C2H5 A-581CH(CH3)CO2CH3 n-C3H7 C2H5 A-582 C(CH3)2OC2CH3 n-C3H7 C2H5 A-583 CH2Phn-C3H7 C2H5 A-584 CH2(3-CF3-Ph) n-C3H7 C2H5 A-585 n-C3H7 i-C3H7 CH3A-586 i-C3H7 i-C3H7 CH3 A-587 CH2CH═CH2 i-C3H7 CH3 A-588 CH2C(CH3)═CH2i-C3H7 CH3 A-589 CH2C(CH3)═CHCH3 i-C3H7 CH3 A-590 CH2CH═C(CH3)2 i-C3H7CH3 A-591 CH2CO2CH3 i-C3H7 CH3 A-592 CH(CH3)CO2CH3 i-C3H7 CH3 A-593C(CH3)2CO2CH3 i-C3H7 CH3 A-594 CH2Ph i-C3H7 CH3 A-595 CH2(3-CF3-Ph)i-C3H7 CH3 A-596 n-C3H7 i-C3H7 C2H5 A-597 i-C3H1 i-C3H7 C2H5 A-598CH2CH═CH2 i-C3H7 C2H5 A-599 CH2C(CH3)═CH2 i-C3H7 C2H5 A-600CH2C(CH3)═CHCH3 i-C3H7 C2H5 A-601 CH2CH═C(CH3)2 t-C3H7 C2H5 A-602CH2OC2CH3 i-C3H7 C2H5 A-603 CH(CH3)CO2CH3 i-C3H7 C2H5 A-604C(CH3)2OC2CH3 i-C3H7 C2H5 A-605 CH2Ph i-C3H7 C2H5 A-606 CH2(3-CF3-Ph)i-C3H7 C2H5 A-607 n-C3H7 n-C4H9 CH3 A-608 i-C3H7 n-C4H9 CH3 A-609CH2CH═CH n-C4H9 CH3 A-610 CH2C(CH3)═CH2 n-C4H9 CH3 A-611 CH2C(CH3)═CHCH3n-C4H9 CH3 A-612 CH2CH═C(CH3)2 n-C4H9 CH3 A-613 CH2OC2CH3 n-C4H9 CH3A-614 CH(CH3)CO2CH3 n-C4H9 CH3 A-615 C(CH3)2CO2CH3 n-C4H9 CH3 A-616CH2Ph n-C4H9 CH3 A-617 CH2(3-CF3-Ph) n-C4H9 CH3 A-618 n-C3H7 CH2CH2OCH3H A-619 i-C3H7 CH2CH2OCH3 H A-620 CH2CH═CH2 CH2CH2OCH3 H A-621CH2C(CH3)═CH2 CH2CH2OCH3 H A-622 CH2C(CH3)═CHCH3 CH2CH2OCH3 H A-623CH2CH═C(CH3)2 CH2CH2OCH3 H A-624 CH2Ph CH2CH2OCH3 H A-625 CH2(3-CF3-Ph)CH2CH2OCH3 H A-626 n-C3H7 CH2CH2OC2H5 H A-627 i-C3H7 CH2CH2OC2H5 H A-628CH2CH═CH CH2CH2OC2H5 H A-629 CH2C(CH3)═CH2 CH2OH2OC2H5 H A-630CH2C(CH3)═CHCH3 CH2CH2OC2H5 H A-631 CH2CH═C(CH3)2 CH2CH2OC2H5 H A-632CH2Ph CH2CH2OC2H5 H A-633 CH2(3-CF3-Ph) CH2CH2OC2H5 H A-634 n-C3H7CH2CH2OC2H4CH3 H A-635 i-C3H7 CH2CH2OC2H4CH3 H A-636 CH2CH═CH2CH2CH2OC2H4CH3 H A-637 CH2C(CH3)═CH2 CH2CH2OC2H4CH3 H A-638CH2C(CH3)═CHCH3 CH2CH2OC2H4CH3 H A-639 CH2CH═C(CH3)2 CH2CH2OC2H4CH3 HA-640 CH2Ph CH2CH2OC2H4CH3 H A-641 CH2(3-CF3-Ph) CH2CH2OC2H4CH3 H A-642n-C3H7 CH2CH2OC3H7CH3 H A-643 i-C3H7 CH2CH2OC3H7CH3 H A-644 CH2CH═CHCH2CH2OC3H7CH3 H A-645 CH2C(CH3)═CH2 CH2CH2OC3H7CH3 H A-646CH2C(CH3)═CHCH3 CH2CH2OC3H7CH3 H A-647 CH2CH═C(CH3)2 CH2CH2OC3H7CH3 HA-648 CH2Ph CH2CH2OC3H7CH3 H A-649 CH2(3-CF3-Ph) CH2CH2OC3H7CH3 H A-650n-C3H7 CH2CF3 H A-651 i-C3H7 CH2CF3 H A-652 CH2CH═CH2 CH2CF3 H A-653CH2C(CH3)═CH2 CH2CF3 H A-654 CH2C(CH3)═CHCH3 CH2CF3 H A-655CH2CH═C(CH3)2 CH2CF3 H A-656 CH2Ph CH2CF3 H A-657 CH2(3-CF3-Ph) CH2CF3 HA-658 n-C3H7 CH2CN H A-659 i-C3H7 CH2CN H A-650 CH2CH═CH2 CH2CN H A-661CH2C(CH3)═CH2 CH2CN H A-662 CH2C(CH3)═CHCH3 CH2CN H A-663 CH2CH═C(CH3)2CH2CN H A-664 CH2Ph CH2CN H A-665 CH2(3-CF3-Ph) CH2CN H A-666 n-C3H7C(CH3)2CN H A-667 i-C3H7 C(CH3)2CN H A-668 CH2CH═CH2 C(CH3)2CN H A-669CH2C(CH3)═CH2 C(CH3)2CN H A-670 CH2C(CH3)═CHCH3 C(CH3)2CN H A-671CH2CH═C(CH3)2 C(CH3)2CN H A-672 CH2Ph C(CH3)2CN H A-673 CH2(3-CF3-Ph)C(CH3)2CN H A-674 n-C3H7 C(CH3)(i-C3H7)CN H A-675 i-C3H7C(CH3)(i-C3H7)CN H A-676 CH2CH═CH C(CH3)(i-C3H7)CN H A-677 CH2C(CH3)═CH2C(CH3)(i-C3H7)CN H A-678 CH2C(CH3)═CHCH3 C(CH3)(i-C3H7)CN H A-679CH2CH═C(CH3)2 C(CH3)(i-C3H7)CN H A-680 CH2Ph C(CH3)(i-C3H7)CN H A-681CH2(3-CF3-Ph) C(CH3)(i-C3H7)CN H A-682 n-C3H7 CH2CH═CH2 H A-683 i-C3H7CH2CH═CH2 H A-684 CH2CH═CH2 CH2CH═CH2 H A-685 CH2C(CH3)═CH2 CH2CH═CH2 HA-686 CH2C(CH3)═CHCH3 CH2CH═CH2 H A-687 CH2CH═C(CH3)2 CH2CH═CH2 H A-688CH2Ph CH2CH═CH2 H A-689 CH2(3-CF3-Ph) CH2CH═CH2 H A-690 n-C3H7CH2C(CH3)═CH2 H A-691 i-C3H7 CH2C(CH3)═CH2 H A-692 CH2CH═CH2CH2C(CH3)═CH2 H A-693 CH2C(CH3)═CH2 CH2C(CH3)═CH2 H A-694CH2C(CH3)═CHCH3 CH2C(CH3)═CH2 H A-695 CH2CH═C(CH3)2 CH2C(CH3)═CH2 HA-696 CH2Ph CH2C(CH3)═CH2 H A-697 CH2(3-CF3-Ph) CH2C(CH3)═CH2 H A-698n-C3H7 CH2CH═CHCH3 H A-699 i-C3H7 CH2CH═CHCH3 H A-700 CH2CH═CH2CH2CH═CHCH3 H A-701 CH2C(CH3)═CH2 CH2CH═CHCH3 H A-702 CH2C(CH3)═CHCH3CH2CH═CHCH3 H A-703 CH2CH═C(CH3)2 CH2CH═CHCH3 H A-704 CH2Ph CH2CH═CHCH3H A-705 CH2(3-CF3-Ph) CH2CH═CHCH3 H A-706 n-C3H7 CH2CCH H A-707 i-C3H7CH2CCH H A-708 CH2CH═CH2 CH2CCH H A-709 CH2C(CH3)═CH2 CH2CCH H A-710CH2C(CH3)═CHCH3 CH2CCH H A-711 CH2CH═C(CH3)2 CH2CCH H A-712 CH2Ph CH2CCHH A-713 CH2(3-CF3-Ph) CH2CCH H A-714 CH3 CH2Ph H A-715 C2H5 CH2Ph HA-716 n-C3H7 CH2Ph H A-717 i-C3H7 CH2Ph H A-718 n-C4H9 CH2Ph H A-719s-C4H9 CH2Ph H A-720 i-C4H9 CH2Ph H A-721 t-C4H9 CH2Ph H A-722 n-C5H11CH2Ph H A-723 n-C6H13 CH2Ph H A-724 CH2CH═CH2 CH2Ph H A-725CH2C(CH3)═CH2 CH2Ph H A-726 CH2CH═CHCH3 CH2Ph H A-727 CH2CH═C(CH3)2CH2Ph H A-728 CH2CCl═CH2 CH2Ph H A-729 CH2CH═CCl2 CH2Ph H A-730CH2CH═CHCF3 CH2Ph H A-731 CH2CH═CHPh CH2Ph H A-732 CH(CH3)CH═CH2 CH2Ph HA-733 CH2CCH CH2Ph H A-734 CH2CCCH3 CH2Ph H A-735 CH2CF3 CH2Ph H A-736CH2CH2OCH3 CH2Ph H A-737 CH2CH2OC2H5 CH2Ph H A-738 CH2CH2CH2OCH3 CH2Ph HA-739 CH2CH2CH2OC2H5 CH2Ph H A-740 CH2CH(OC2H5)2 CH2Ph H A-741 CH2CNCH2Ph H A-742 CH2(cyclo-C3H5) CH2Ph H A-743 CH2(cyclo-C5H9) CH2Ph HA-744 CH2(cyclo-C6H11) CH2Ph H A-745 CH2Ph CH2Ph H A-746 CH2(2-Cl-Ph)CH2Ph H A-747 CH2(3-Cl-Ph) CH2Ph H A-748 CH2(4-Cl-Ph) CH2Ph H A-749CH2(2-CF3-Ph) CH2Ph H A-750 CH2(3-CF3-Ph) CH2Ph H A-751 CH2(4-CF3-Ph)CH2Ph H A-752 CH2(2-F-Ph) CH2Ph H A-753 CH2(3-F-Ph) CH2Ph H A-754CH2(4-F-Ph) CH2Ph H A-755 CH2(2-OMe-Ph) CH2Ph H A-756 CH2(3-OMe-Ph)CH2Ph H A-757 CH2(4-OMe-Ph) CH2Ph H A-758 CH(CH3)Ph CH2Ph H A-759CH(CH3)(2-Cl-Ph) CH2Ph H A-760 CH(CH3)(3-Cl-Ph) CH2Ph H A-761CH(CH3)(4-Cl-Ph) CH2Ph H A-762 CH(CH3)(2-CF3-Ph) CH2Ph H A-763CH(CH3)(3-CF3-Ph) CH2Ph H A-764 CH(CH3)(4-CF3-Ph) CH2Ph H A-765 CH2CH2PhCH2Ph H A-766 CH3 CH2Ph CH3 A-767 C2H5 CH2Ph CH3 A-768 n-C3H7 CH2Ph CH3A-769 i-C3H7 CH2Ph CH3 A-770 n-C4H9 CH2Ph CH3 A-771 s-C4H9 CH2Ph CH3A-772 i-C4H9 CH2Ph CH3 A-773 t-C4H9 CH2Ph CH3 A-774 n-C5H11 CH2Ph CH3A-775 n-C6H13 CH2Ph CH3 A-776 CH2CH═CH2 CH2Ph CH3 A-777 CH2C(CH3)═CH2CH2Ph CH3 A-778 CH2C(CH3)═CHCH3 CH2Ph CH3 A-779 CH2CH═C(CH3)2 CH2Ph CH3A-780 CH2CCl═CH2 CH2Ph CH3 A-781 CH2CH═CCl2 CH2Ph CH3 A-782 CH2CH═CHCF3CH2Ph CH3 A-783 CH2CH═CHPh CH2Ph CH3 A-784 CH(CH3)CH═CH2 CH2Ph CH3 A-785CH2CCH CH2Ph CH3 A-786 CH2CCCH3 CH2Ph CH3 A-787 CH2CF3 CH2Ph CH3 A-788CH2CH2OCH3 CH2Ph CH3 A-789 CH2CH2OC2H5 CH2Ph CH3 A-790 CH2CH2CH2OCH3CH2Ph CH3 A-791 CH2CH2CH2OC2H5 CH2Ph CH3 A-792 CH2CH(OCH3)2 CH2Ph CH3A-793 CH2CN CH2Ph CH3 A-794 CH2(cyclo-C3H5) CH2Ph CH3 A-795CH2(cyclo-C5H9) CH2Ph CH3 A-796 CH2(cyclo-C6H11) CH2Ph CH3 A-797CH2CO2CH3 CH2Ph CH3 A-798 CH2CO2C2H5 CH2Ph CH3 A-799 CH(CH3)CO2CH3 CH2PhCH3 A-800 CH(CH3)CO2C2H5 CH2Ph CH3 A-801 C(CH3)2OC2CH3 CH2Ph CH3 A-802C(CH3)2CO2C2H5 CH2Ph CH3 A-803 CH2Ph CH2Ph CH3 A-804 CH2(2-Cl-Ph) CH2PhCH3 A-805 CH2(3-Cl-Ph) CH2Ph CH3 A-8C6 CH2(4-Cl-Ph) CH2Ph CH3 A-807CH2(2-CF3-Ph) CH2Ph CH3 A-808 CH2(3-CF3-Ph) CH2Ph CH3 A-809CH2(4-CF3-Ph) CH2Ph CH3 A-810 CH2(2-F-Ph) CH2Ph CH3 A-811 CH2(3-F-Ph)CH2Ph CH3 A-812 CH2(4-F-Ph) CH2Ph CH3 A-813 CH2(2-OMe-Ph) CH2Ph CH3A-814 CH2(3-OMe-Ph) CH2Ph CH3 A-815 CH2(4-OMe-Ph) CH2Ph CH3 A-816CH(CH3)Ph CH2Ph CH3 A-817 CH(CH3)(2-Cl-Ph) CH2Ph CH3 A-818CH(CH3)(3-Cl-Ph) CH2Ph CH3 A-819 CH(CH3)(4-Cl-Ph) CH2Ph CH3 A-820CH(CH3)(2-CF3-Ph) CH2Ph CH3 A-821 CH(CH3)(3-CF3-Ph) CH2Ph CH3 A-822CH(CH3)(4-CF3-Ph) CH2Ph CH3 A-823 CH2CH2Ph CH2Ph CH3 A-824 n-C3H7CH2(2-OMe-Ph) H A-825 i-C3H7 CH2(2-OMe-Ph) H A-826 CH2CH═CHCH2(2-OMe-Ph) H A-827 CH2C(CH3)═CH2 CH2(2-OMe-Ph) H A-828CH2C(CH3)═CHCH3 CH2(2-OMe-Ph) H A-829 CH2CH═C(CH3)2 CH2(2-OMe-Ph) HA-830 CH2Ph CH2(2-OMe-Ph) H A-831 CH2(3-CF3-Ph) CH2(2-OMe-Ph) H A-832n-C3H7 CH2(3-OMe-Ph) H A-833 i-C3H7 CH2(3-OMe-Ph) H A-834 CH2CH═CH2CH2(3-OMe-Ph) H A-835 CH2C(CH3)═CH2 CH2(3-OMe-Ph) H A-836CH2C(CH3)═CHCH3 CH2(3-OMe-Ph) H A-837 CH2CH═C(CH3)2 CH2(3-OMe-Ph) HA-838 CH2Ph CH2(3-OMe-Ph) H A-839 CH2(3-CF3-Ph) CH2(3-OMe-Ph) H A-840n-C3H7 CH2(4-OMe-Ph) H A-841 i-C3H7 CH2(4-OMe-Ph) H A-842 CH2CH═CHCH2(4-OMe-Ph) H A-843 CH2C(CH3)═CH2 CH2(4-OMe-Ph) H A-844CH2C(CH3)═CHCH3 CH2(4-OMe-Ph) H A-845 CH2CH═C(CH3)2 CH2(4-OMe-Ph) HA-846 CH2Ph CH2(4-OMe-Ph) H A-847 CH2(3-CF3-Ph) CH2(4-OMe-Ph) H A-848n-C3H7 CH2(2-Cl-Ph) H A-849 i-C3H7 CH2(2-Cl-Ph) I-i A-850 CH2CH═CH2CH2(2-Cl-Ph) H A-851 CH2C(CH3)═CH2 CH2(2-Cl-Ph) H A-852 CH2C(CH3)═CHCH3CH2(2-Cl-Ph) H A-853 CH2CH═C(CH3)2 CH2(2-Cl-Ph) H A-854 CH2PhCH2(2-Cl-Ph) H A-855 CH2(3-CF3-Ph) CH2(2-Cl-Ph) H A-856 n-C3H7CH2(3-Cl-Ph) H A-857 i-C3H7 CH2(3-Cl-Ph) H A-858 CH2CH═CH2 CH2(3-Cl-Ph)H A-859 CH2C(CH3)═CH2 CH2(3-Cl-Ph) H A-860 CH2C(CH3)═CHCH3 CH2(3-Cl-Ph)H A-861 CH2CH═C(CH3)2 CH2(3-Cl-Ph) H A-862 CH2Ph CH2(3-Cl-Ph) H A-863CH2(3-CF3-Ph) CH2(3-Cl-Ph) H A-864 n-C3H7 CH2(4-Cl-Ph) H A-865 i-C3H7CH2(4-Cl-Ph) H A-866 CH2CH═CH CH2(4-Cl-Ph) H A-867 CH2C(CH3)═CH2CH2(4-Cl-Ph) H A-868 CH2C(CH3)═CHCH3 CH2(4-Cl-Ph) H A-869 CH2CH═C(CH3)2CH2(4-Cl-Ph) H A-870 CH2Ph CH2(4-Cl-Ph) H A-871 CH2(3-CF3-Ph)CH2(4-Cl-Ph) H A-872 n-C3H7 CH2(2-CF3-Ph) H A-873 i-C3H7 CH2(2-CF3-Ph) HA-874 CH2CH═CH2 CH2(2-CF3-Ph) H A-875 CH2C(CH3)═CH2 CH2(2-CF3-Ph) HA-876 CH2C(CH3)═CHCH3 CH2(2-CF3-Ph) H A-877 CH2CH═C(CH3)2 CH2(2-CF3-Ph)H A-878 CH2Ph CH2(2-CF3-Ph) H A-879 CH2(3-CF3-Ph) CH2(2-CF3-Ph) H A-880n-C3H7 CH2(3-CF3-Ph) H A-881 i-C3H7 CH2(3-CF3-Ph) H A-882 CH2CH═CH2CH2(3-CF3-Ph) H A-883 CH2C(CH3)═CH2 CH2(3-CF3-Ph) H A-884CH2C(CH3)═CHCH3 CH2(3-CF3-Ph) H A-885 CH2CH═C(CH3)2 CH2(3-CF3-Ph) HA-886 CH2Ph CH2(3-CF3-Ph) H A-887 CH2(3-CF3-Ph) CH2(3-CF3-Ph) H A-888n-C3H7 CH2(4-CF3-Ph) H A-889 i-C3H7 CH2(4-CF3-Ph) H A-890 CH2CH═CH2CH2(4-CF3-Ph) H A-891 CH2C(CH3)═CH2 CH2(4-CF3-Ph) H A-892CH2C(CH3)═CHCH3 CH2(4-CF3-Ph) H A-893 CH2CH═C(CH3)2 CH2(4-CF3-Ph) HA-894 CH2Ph CH2(4-CF3-Ph) H A-895 CH2(3-CF3-Ph) CH2(4-CF3-Ph) H A-896CH3 cyclo-C3H5 H A-897 C2H5 cyclo-C3H5 H A-898 n-C3H7 cyclo-C3H5 H A-899i-C3H7 cyclo-C3H5 H A-900 n-C4H9 cyclo-C3H5 H A-901 s-C4H9 cyclo-C3H5 HA-902 n-C5H11 cyclo-03H5 H A-903 n-C6H13 cyclo-C3H5 H A-904 CH2CH═CH2cyclo-C3H5 H A-905 CH2C(CH3)═CH2 cyclo-C3H5 H A-906 CH2C(CH3)═CHCH3cyclo-C3H5 H A-907 CH2CH═C(CH3)2 cyclo-C3H5 H A-908 CH2CCl═CH2cyclo-C3H5 H A-909 CH2CH═CCl2 cyclo-C3H5 H A-910 CH2CH═CHCF3 cyclo-C3H5H A-911 CH(CH3)CH═CH2 cyclo-C3H5 H A-912 CH2CCCH3 cyclo-C3H5 H A-913CH2CF3 cyclo-C3H5 H A-914 CH2CH2OCH3 cyclo-C3H5 H A-915 CH2CH2OC2H5cyclo-C3H5 H A-916 CH2CH2CH2OCH3 cyclo-C3H5 H A-917 CH2CH2CH2OC2H5cyclo-C3H5 H A-918 CH2CH(OCH3)2 cyclo-C3H5 H A-919 CH2Ph cyclo-C3H5 HA-920 CH2(2-Cl-Ph) cyclo-C3H5 H A-921 CH2(3-Cl-Ph) cyclo-C3H5 H A-922CH2(4-Cl-Ph) cyclo-C3H5 H A-923 CH2(2-CF3-Ph) cyclo-C3H5 H A-924CH2(3-CF3-Ph) cyclo-C3H5 H A-925 CH2(4-CF3-Ph) cyclo-C3H5 H A-926CH(CH3)Ph cyclo-C3H5 H A-927 CH3 cyclo-C5H9 H A-928 C2H5 cyclo-C5H9 HA-929 n-C3H7 cyclo-C5H9 H A-930 i-C3H7 cyclo-C5H9 H A-931 n-C4H9cyclo-C5H9 H A-932 s-C4H9 cyclo-C5H9 H A-933 n-C5H11 cyclo-C5H9 H A-934n-C6H13 cyclo-C5H9 H A-935 CH2CH═CH cyclo-C5H9 H A-936 CH2C(CH3)═CH2cyclo-C5H9 H A-937 CH2C(CH3)═CHCH3 cyclo-C5H9 H A-938 CH2CH═C(CH3)2cyclo-C5H9 H A-939 CH2CCl═CH2 cyclo-C5H9 H A-940 CH2CH═CCl2 cyclo-C5H9 HA-941 CH2CH═CHCF3 cyclo-C5H9 H A-942 CH(CH3)CH═CH2 cyclo-C5H9 H A-943CH2CCCH3 cyclo-C5H9 H A-944 CH2CF3 cyclo-C5H9 H A-945 CH2CH2OCH3cyclo-C5H9 H A-946 CH2CH2OC2H5 cyclo-C5H9 H A-947 CH2CH2CH2OCH3cyclo-C5H9 H A-948 CH2CH2CH2OC2H5 cyclo-C5H9 H A-949 CH2CH(OCH3)2cyclo-C5H9 H A-950 CH2Ph cyclo-C5H9 H A-951 CH2(2-Cl-Ph) cyclo-C5H9 HA-952 CH2(3-Cl-Ph) cyclo-C5H9 H A-953 CH2(4-Cl-Ph) cyclo-C5H9 H A-954CH2(2-CF3-Ph) cyclo-C5H9 H A-955 CH2(3-CF3-Ph) cyclo-C5H9 H A-956CH2(4-CF3-Ph) cyclo-C5H9 H A-957 CH(CH3)Ph cyclo-C5H9 H A-958 CH3cyclo-C6H11 H A-959 C2H5 cyclo-C6H11 H A-960 n-C3H7 cyclo-C6H11 H A-961i-C3H7 cyclo-C6H11 H A-962 n-C4H9 cyclo-C6H11 H A-963 s-C4H9 cyclo-C6H11H A-964 n-C5H11 cyclo-C6H11 H A-965 n-C6H13 cyclo-C6H11 H A-966 CH2CH═CHcyclo-C6H11 H A-967 CH2C(CH3)═CH2 cyclo-C6H11 H A-968 CH2C(CH3)═CHCH3cyclo-C6H11 H A-969 CH2CH═C(CH3)2 cyclo-C6H11 H A-970 CH2CCl═CH2cyclo-C6H11 H A-971 CH2CH═CCl2 cyclo-C6H11 H A-972 CH2CH═CHCF3cyclo-C6H11 H A-973 CH(CH3)CH═CH2 cyclo-C6H11 H A-974 CH2CCCH3cyclo-C6H11 H A-975 CH2CF3 cyclo-C6H11 H A-976 CH2CH2OCH3 cyclo-C6H11 HA-977 CH2CH2OC2H5 cyclo-C6H11 H A-978 CH2CH2CH2OCH3 cyclo-C6H11 H A-979CH2CH2CH2OC2H5 cyclo-C6H11 H A-980 CH2CH(OCH3)2 cyclo-C6H11 H A-981CH2Ph cyclo-C6H11 H A-982 CH2(2-Cl-Ph) cyclo-C6H11 H A-983 CH2(3-Cl-Ph)cyclo-C6H11 H A-984 CH2(4-Cl-Ph) cyclo-C6H11 H A-985 CH2(2-CF3-Ph)cyclo-C6H11 H A-986 CH2(3-CF3-Ph) cyclo-C6H11 H A-987 CH2(4-CF3-Ph)cyclo-C6H11 H A-988 CH(CH3)Ph cyclo-C6H11 H A-989 CH3 cyclo-C6H11 CH3A-990 C2H5 cyclo-C6H11 CH3 A-991 n-C3H7 cyclo-C6H11 CH3 A-992 i-C3H7cyclo-C6H11 CH3 A-993 n-C4H9 cyclo-C6H11 CH3 A-994 s-C4H9 cyclo-C6H11CH3 A-995 n-C5H11 cyclo-C6H11 CH3 A-996 n-C6H13 cyclo-C6H11 CH3 A-997CH2CH═CH cyclo-C6H11 CH3 A-998 CH2C(CH3)═CH2 cyclo-C6H11 CH3 A-999CH2C(CH3)═CHCH3 cyclo-C6H11 CH3 A-1000 CH2CH═C(CH3)2 cyclo-C6H11 CH3A-1001 CH2CCl═CH2 cyclo-C6H11 CH3 A-1002 CH2CH═CCl2 cyclo-C6H11 CH3A-1003 CH2CH═CHCF3 cyclo-C6H11 CH3 A-1004 CH(CH3)CH═CH2 cyclo-C6H11 CH3A-1005 CH2CCCH3 cyclo-C6H11 CH3 A-1006 CH2CF3 cyclo-C6H11 CH3 A-1007CH2CH2OCH3 cyclo-C6H11 CH3 A-1008 CH2CH2OC2H5 cyclo-C6H11 CH3 A-1009CH2CH2CH2OCH3 cyclo-C6H11 CH3 A-1010 CH2CH2CH2OC2H5 cyclo-C6H11 CH3A-1011 CH2CH(OCH3)2 cyclo-O6H11 CH3 A-1012 CH2CO2CH3 cyclo-C6H11 CH3A-1013 CH2OC2C2H5 cyclo-C6H11 CH3 A-1014 CH(CH3)CO2CH3 cyclo-C6H11 CH3A-1015 CH(CH3)CO2C2H5 cyclo-C6H11 CH3 A-1016 C(CH3)2OC2CH3 cyclo-C6H11CH3 A-1017 C(CH3)2CO2C2H5 cyclo-C6H11 CH3 A-1018 CH2Ph cyclo-C6H11 CH3A-1019 CH2(2-Cl-Ph) cyclo-C6H11 CH3 A-1020 CH2(3-Cl-Ph) cyclo-C6H11 CH3A-1021 CH2(4-Cl-Ph) cyclo-C6H11 CH3 A-1022 CH2(2-CF3-Ph) cyclo-C6H11 CH3A-1023 CH2(3-CF3-Ph) cyclo-C6H11 CH3 A-1024 CH2(4-CF3-Ph) cyclo-C6H11CH3 A-1025 CH(CH3)Ph cyclo-C6H11 CH3 A-1026 CH3 cyclo-C6H11 C2H5 A-1027C2H5 cyclo-C6H11 C2H5 A-1028 n-C3H7 cyclo-C6H11 C2H5 A-1029 i-C3H7cyclo-C6H11 C2H5 A-1030 n-C4H9 cyclo-C6H11 C2H5 A-1031 s-C4H9cyclo-C6H11 C2H5 A-1032 n-C5H11 cyclo-C6H11 C2H5 A-1033 n-C6H13cyclo-C6H11 C2H5 A-1034 CH2CH═CH cyclo-C6H11 C2H5 A-1035 CH2C(CH3)═CH2cyclo-C6H11 C2H5 A-1036 CH2C(CH3)═CHCH3 cyclo-C6H11 C2H5 A-1037CH2CH═C(CH3)2 cyclo-C6H11 C2H5 A-1038 CH2CCl═CH2 cyclo-C6H11 C2H5 A-1039CH2CH═CCl2 cyclo-C6H11 C2H5 A-1040 CH2CH═CHCF3 cyclo-C6H11 C2H5 A-1041CH(CH3)CH═CH2 cyclo-C6H11 C2H5 A-1042 CH2CCCH3 cyclo-C6H11 C2H5 A-1043CH2CF3 cyclo-C6H11 C2H5 A-1044 CH2CH2OCH3 cyclo-C6H11 C2H5 A-1045CH2CH2OC2H5 cyclo-C6H11 C2H5 A-1046 CH2CH2CH2OCH3 cyclo-C6H11 C2H5A-1047 CH2CH2CH2OC2H5 cyclo-C6H11 C2H5 A-1048 CH2CH(OCH3)2 cyclo-C6H11C2H5 A-1049 CH2OC2CH3 cyclo-C6HlI C2H5 A-1050 CH2OC2C2H5 cyclo-C6H11C2H5 A-1051 CH(CH3)CO2CH3 cyclo-C6H11 C2H5 A-1052 CH(CH3)CO2C2H5cyclo-C6H11 C2H5 A-1053 C(CH3)2OC2CH3 cyclo-C6HlI C2H5 A-1054C(CH3)2CO2C2H5 cyclo-C6H11 C2H5 A-1055 CH2Ph cyclo-C6H11 C2H5 A-1056CH2(2-Cl-Ph) cyclo-C6H11 C2H5 A-1057 CH2(3-Cl-Ph) cyclo-C6H11 C2H5A-1058 CH2(4-Cl-Ph) cyclo-C6H11 C2H5 A-1059 CH2(2-CF3-Ph) cyclo-C6H11C2H5 A-1060 CH2(3-CF3-Ph) cyclo-C6H11 C2H5 A-1061 CH2(4-CF3-Ph)cyclo-C6H11 C2H5 A-1062 CH(CH3)Ph cyclo-C6H11 C2H5 A-1063 CH3 (CH2)4A-1064 C2H5 (CH2)4 A-1065 n-C3H7 (CH2)4 A-1066 i-C3H7 (CH2)4 A-1067n-C4H9 (CH2)4 A-1068 s-C4H9 (CH2)4 A-1069 n-C5H11 (CH2)4 A-1070 n-C6H13(CH2)4 A-1071 CH2CH═CH2 (CH2)4 A-1072 CH2C(CH3)═CH2 (CH2)4 A-1073CH2C(CH3)═CHCH3 (CH2)4 A-1074 CH2CH═C(CH3)2 (CH2)4 A-1075 CH2CCl═CH2(CH2)4 A-1076 CH2CH═CCl2 (CH2)4 A-1077 CH2CH═CHCF3 (CH2)4 A-1078CH(CH3)CH═CH2 (CH2)4 A-1079 CH2CCCH3 (CH2)4 A-1080 CH2CF3 (CH2)4 A-1081CH2CH2OCH3 (CH2)4 A-1082 CH2CH2OC2H5 (CH2)4 A-1083 CH2CH2CH2OCH3 (CH2)4A-1084 CH2CH2CH2OC2H5 (CH2)4 A-1085 CH2CH(OCH3)2 (CH2)4 A-1086 CH2CO2CH3(CH2)4 A-1087 CH2OC2C2H5 (CH2)4 A-1088 CH(CH3)CO2CH3 (CH2)4 A-1089CH(CH3)CO2C2H5 (CH2)4 A-1090 C(CH3)2OC2CH3 (CH2)4 A-1091 C(CH3)2OC2C2H5(CH2)4 A-1092 CH2Ph (CH2)4 A-1093 CH2(2-Cl-Ph) (CH2)4 A-1094CH2(3-Cl-Ph) (CH2)4 A-1095 CH2(4-Cl-Ph) (CH2)4 A-1096 CH2(2-CF3-Ph)(CH2)4 A-1097 CH2(3-CF3-Ph) (CH2)4 A-1098 CH2(4-CF3-Ph) (CH2)4 A-1099CH(CH3)Ph (CH2)4 A-1100 CH3 (CH2)5 A-1101 C2H5 (CH2)5 A-1102 n-C3H7(CH2)5 A-1103 i-C3H7 (CH2)5 A-1104 n-C4H9 (CH2)5 A-1105 s-C4H9 (CH2)5A-1106 n-C5H11 (CH2)5 A-1107 n-C6H13 (CH2)5 A-1108 CH2CH═CH2 (CH2)5A-1109 CH2C(CH3)═CH2 (CH2)5 A-1110 CH2C(CH3)═CHCH3 (CH2)5 A-1111CH2CH═C(CH3)2 (CH2)5 A-1112 CH2CCl═CH2 (CH2)5 A-1113 CH2CH═CCl2 (CH2)5A-1114 CH2CH═CHCF3 (CH2)5 A-1115 CH(CH3)CH═CH2 (CH2)5 A-1116 CH2CCCH3(CH2)5 A-1117 CH2CF3 (CH2)5 A-1118 CH2CH2OCH3 (CH2)5 A-1119 CH2CH2OC2H5(CH2)5 A-1120 CH2CH2CH2OCH3 (CH2)5 A-1121 CH2CH2CH2OC2H5 (CH2)5 A-1122CH2CH(OCH3)2 (CH2)5 A-1123 CH2CO2CH3 (CH2)5 A-1124 CH2OC2C2H5 (CH2)5A-1125 CH(CH3)CO2CH3 (CH2)5 A-1126 CH(CH3)CO2C2H5 (CH2)5 A-1127C(CH3)2CO2CH3 (CH2)5 A-1128 C(CH3)2OC2C2H5 (CH2)5 A-1129 CH2Ph (CH2)5A-1130 CH2(2-Cl-Ph) (CH2)5 A-1131 CH2(3-Cl-Ph) (CH2)5 A-1132CH2(4-Cl-Ph) (CH2)5 A-1133 CH2(2-CF3-Ph) (CH2)5 A-1134 CH2(3-CF3-Ph)(CH2)5 A-1135 CH2(4-CF3-Ph) (CH2)5 A-1136 CH(CH3)Ph CH2CH2OCH2CH2 A-1137CH3 CH2CH2OCH2CH2 A-1138 C2H5 CH2CH2OCH2CH2 A-1139 n-C3H7 CH2CH2OCH2CH2A-1140 i-C3H7 CH2CH2OCH2CH2 A-1141 n-C4H9 CH2CH2OCH2CH2 A-1142 s-C4H9CH2CH2OCH2CH2 A-1143 n-C5H11 CH2CH2OCH2CH2 A-1144 n-C6H13 CH2CH2OCH2CH2A-1145 CH2CH═CH CH2CH2OCH2CH2 A-1146 CH2C(CH3)═CH2 CH2CH2OCH2CH2 A-1147CH2C(CH3)═CHCH3 CH2CH2OCH2CH2 A-1148 CH2CH═C(CH3)2 CH2CH2OCH2CH2 A-1149CH2CCl═CH2 CH2CH2OCH2CH2 A-1150 CH2CH═CCl2 CH2CH2OCH2CH2 A-1151CH2CH═CHCF3 CH2CH2OCH2CH2 A-1152 CH(CH3)CH═CH2 CH2CH2OCH2CH2 A-1153CH2CCCH3 CH2CH2OCH2CH2 A-1154 CH2CF3 CH2CH2OCH2CH2 A-1155 CH2CH2OCH3CH2CH2OCH2CH2 A-1156 CH2CH2OC2H5 CH2CH2OCH2CH2 A-1157 CH2CH2CH2OCH3CH2CH2OCH2CH2 A-1158 CH2CH2CH2OC2H5 CH2CH2OCH2CH2 A-1159 CH2CH(OCH3)2CH2CH2OCH2CH2 A-1160 CH2OC2CH3 CH2CH2OCH2CH2 A-1161 CH2OC2C2H5CH2CH2OCH2CH2 A-1162 CH(CH3)CO2CH3 CH2CH2OCH2CH2 A-1163 CH(CH3)CO2C2H5CH2CH2OCH2CH2 A-1164 C(CH3)2CO2CH3 CH2CH2OCH2CH2 A-1165 C(CH3)2CO2C2H5CH2CH2OCH2CH2 A-1166 CH2Ph CH2CH2OCH2CH2 A-1167 CH2(2-Cl-Ph)CH2CH2OCH2CH2 A-1168 CH2(3-Cl-Ph) CH2CH2OCH2CH2 A-1169 CH2(4-Cl-Ph)CH2CH2OCH2CH2 A-1170 CH2(2-CF3-Ph) CH2CH2OCH2CH2 A-1171 CH2(3-CF3-Ph)CH2CH2OCH2CH2 A-1172 CH2(4-CF3-Ph) CH2CH2OCH2CH2 A-1173 CH(CH3)PhCH2CH2OCH2CH2 A-1174 CH3 CH2CH2SCH2CH2 A-1175 C2H5 CH2CH2SCH2CH2 A-1176n-C3H7 CH2CH2SCH2CH2 A-1177 i-C3H7 CH2CH2SCH2CH2 A-1178 n-C4H9CH2CH2SCH2CH2 A-1179 s-C4H9 CH2CH2SCH2CH2 A-1180 n-C5H11 CH2CH2SCH2CH2A-1181 n-C6H13 CH2CH2SCH2CH2 A-1182 CH2CH═CH2 CH2CH2SCH2CH2 A-1183CH2C(CH3)═CH2 CH2CH2SCH2CH2 A-1184 CH2C(CH3)═CHCH3 CH2CH2SCH2CH2 A-1185CH2CH═C(CH3)2 CH2CH2SCH2CH2 A-1186 CH2CCl═CH2 CH2CH2SCH2CH2 A-1187CH2CH═CCl2 CH2CH2SCH2CH2 A-1188 CH2CH═CHCF3 CH2CH2SCH2CH2 A-1189CH(CH3)CH═CH2 CH2CH2SCH2CH2 A-1190 CH2CCCH3 CH2CH2SCH2CH2 A-1I91 CH2CF3CH2CH2SCH2CH2 A-1192 CH2CH2OCH3 CH2CH2SCH2CH2 A-1193 CH2CH2OC2H5CH2CH2SCH2CH2 A-1194 CH2CH2CH2OCH3 CH2CH2SCH2CH2 A-1195 CH2CH2CH2OC2H5CH2CH2SCH2CH2 A-1196 CH2CH(OCH3)2 CH2CH2SCH2CH2 A-1197 CH2OC2CH3CH2CH2SCH2CH2 A-1198 CH2OC2C2H5 CH2CH2SCH2CH2 A-1199 CH(CH3)CO2CH3CH2CH2SCH2CH2 A-1200 CH(CH3)CO2C2H5 CH2CH2SCH2CH2 A-1201 C(CH3)2CO2CH3CH2CH2SCH2CH2 A-1202 C(CH3)2CO2C2H5 CH2CH2SCH2CH2 A-1203 CH2PhCH2CH2SCH2CH2 A-1204 CH2(2-Cl-Ph) CH2CH2SCH2CH2 A-1205 CH2(3-Cl-Ph)CH2CH2SCH2CH2 A-1206 CH2(4-Cl-Ph) CH2CH2SCH2CH2 A-1207 CH2(2-CF3-Ph)CH2CH2SCH2CH2 A-1208 CH2(3-CF3-Ph) CH2CH2SCH2CH2 A-1209 CH2(4-CF3-Ph)CH2CH2SCH2CH2 A-1210 CH(CH3)Ph CH2CH2SCH2CH2 A-1211 n-C3H7 OCH3 H A-1212i-C3H7 OCH3 H A-1213 CH2CH═CH2 OCH3 H A-1214 CH2C(CH3)═CH2 OCH3 H A-1215CH2C(CH3)═CHCH3 OCH3 H A-1216 CH2CH═C(CH3)2 OCH3 H A-1217 CH2Ph OCH3 HA-1218 CH2(3-CF3-Ph) OCH3 H A-1219 n-C3H7 OC2H5 H A-1220 i-C3H7 OC2H5 HA-1221 CH2CH═CH2 OC2H5 H A-1222 CH2C(CH3)═CH2 OC2H5 H A-1223CH2C(CH3)═CHCH3 OC2H5 H A-1224 CH2CH═C(CH3)2 OC2H5 H A-1225 CH2Ph OC2H5H A-1226 CH2(3-CF3-Ph) OC2H5 H A-1227 n-C3H7 O(i-C3H7) H A-1228 i-C3H7O(i-C3H7) H A-1229 CH2CH═CH2 O(i-C3H7) H A-1230 CH2C(CH3)═CH2 O(i-C3H7)H A-1231 CH2C(CH3)═CHCH3 O(i-C3H7) H A-1232 CH2CH═C(CH3)2 O(i-C3H7) HA-1233 CH2Ph O(i-C3H7) H A-1234 CH2(3-CF3-Ph) O(i-C3H7) H A-1235 n-C3H7O(t-C4H9) H A-1236 i-C3H7 O(t-C4H9) H A-1237 CH2CH═CH2 O(t-C4H9) HA-1238 CH2C(CH3)═CH2 O(t-C4H9) H A-1239 CH2C(CH3)═CHCH3 O(t-C4H9) HA-1240 CH2CH═C(CH3)2 O(t-C4H9) H A-1241 CH2Ph O(t-C4H9) H A-1242CH2(3-CF3-Ph) O(t-C4H9) H A-1243 n-C3H7 OCH3 CH3 A-1244 i-C3H7 OCH3 CH3A-1245 CH2CH═CH2 OCH3 CH3 A-1246 CH2C(CH3)═CH2 OCH3 CH3 A-1247CH2C(CH3)═CHCH3 OCH3 CH3 A-1248 CH2CH═C(CH3)2 OCH3 CH3 A-1249 CH2OC2CH3OCH3 CH3 A-1250 CH(CH3)CO2CH3 OCH3 CH3 A-1251 C(CH3)2OC2CH3 OCH3 CH3A-1252 CH2Ph OCH3 CH3 A-1253 CH2(3-CF3-Ph) OCH3 CH3 A-1254 n-C3H7 OCH2PhH A-1255 i-C3H7 OCH2Ph H A-1256 CH2CH═CH2 OCH2Ph H A-1257 CH2C(CH3)═CH2OCH2Ph H A-1258 CH2C(CH3)═CHCH3 OCH2Ph H A-1259 CH2CH═C(CH3)2 OCH2Ph HA-1260 CH2OC2CH3 OCH2Ph H A-1261 CH(CH3)CO2CH3 OCH2Ph H A-1262C(CH3)2CO2CH3 OCH2Ph H A-1263 CH2Ph OCH2Ph H A-1264 CH2(3-CF3-Ph) OCH2PhH A-1265 n-C3H7 Ph H A-1266 i-C3H7 Ph H A-1267 CH2CH═CH Ph H A-1268CH2C(CH3)═CH2 Ph H A-1269 CH2C(CH3)═CHCH3 Ph H A-1270 CH2CH═C(CH3)2 Ph HA-1271 CH2Ph Ph H A-1272 CH2(3-CF3-Ph) Ph H A-1273 n-C3H7 4-Cl-Ph HA-1274 i-C3H7 4-Cl-Ph H A-1275 CH2CH═CH2 4-Cl-Ph H A-1276 CH2C(CH3)═CH24-Cl-Ph H A-1277 CH2C(CH3)═CHCH3 4-Cl-Ph H A-1278 CH2CH═C(CH3)2 4-Cl-PhH A-1279 CH2Ph 4-Cl-Ph H A-1280 CH2(3-CF3-Ph) 4-Cl-Ph H A-1281 n-C3H74-CH3O-Ph H A-1282 i-C3H7 4-CH3O-Ph H A-1283 CH2CH═CH 4-CH3O-Ph H A-1284CH2C(CH3)═CH2 4-CH3O-Ph H A-1285 CH2C(CH3)═CHCH3 4-CH3O-Ph H A-1286CH2CH═C(CH3)2 4-CH3O-Ph H A-1287 CH2Ph 4-CH3O-Ph H A-1288 CH2(3-CF3-Ph)4-CH3O-Ph H A-1289 n-C3H7 4-CF3CH2O-Ph H A-1290 i-C3H7 4-CF3CH2O-Ph HA-1291 CH2CH═CH 4-CF3CH2O-Ph H A-1292 CH2C(CH3)═CH2 4-CF3CH2O-Ph HA-1293 CH2C(CH3)═CHCH3 4-CF3CH2O-Ph H A-1294 CH2CH═C(CH3)2 4-CF3CH2O-PhH A-1295 CH2Ph 4-CF3CH2O-Ph H A-1296 CH2(3-CF3-Ph) 4-CF3CH2O-Ph H A-1297n-C3H7 4-PhO-Ph H A-1298 i-C3H7 4-PhO-Ph H A-1299 CH2CH═CH 4-PhO-Ph HA-1300 CH2C(CH3)═CH2 4-PhO-Ph H A-1301 CH2C(CH3)═CHCH3 4-PhO-Ph H A-1302CH2CH═C(CH3)2 4-PhO-Ph H A-1303 CH2Ph 4-PhO-Ph H A-1304 CH2(3-CF3-Ph)4-PhO-Ph H A-1305 n-C3H7 4-(4-Cl-Ph)O-Ph H A-13C6 i-C3H7 4-(4-Cl-Ph)O-PhH A-1307 CH2CH═CH 4-(4-Cl-Ph)O-Ph H A-1308 CH2C(CH3)═CH2 4-(4-Cl-Ph)O-PhH A-1309 CH2C(CH3)═CHCH3 4-(4-Cl-Ph)O-Ph H A-1310 CH2CH═C(CH3)24-(4-Cl-Ph)O-Ph H A-1311 CH2Ph 4-(4-Cl-Ph)O-Ph H A-1312 CH2(3-CF3-Ph)4-(4-Cl-Ph)O-Ph H A-1313 n-C3H7 4-(4-CF3-Ph)O-Ph H A-1314 i-C3H74-(4-CF3-Ph)O-Ph H A-1315 CH2CH═CH 4-(4-CF3-Ph)O-Ph H A-1316CH2C(CH3)═CH2 4-(4-CF3-Ph)O-Ph H A-13I7 CH2C(CH3)═CHCH3 4-(4-CF3-Ph)O-PhH A-1318 CH2CH═C(CH3)2 4-(4-CF3-Ph)O-Ph H A-1319 CH2Ph 4-(4-CF3-Ph)O-PhH A-1320 CH2(3-CF3-Ph) 4-(4-CF3-Ph)O-Ph H A-1321 CH3 Ph CH3 A-1322 C2H5Ph CH3 A-1323 n-C3H7 Ph CH3 A-1324 i-C3H7 Ph CH3 A-1325 CH2CH═CH Ph CH3A-1326 CH2C(CH3)═CH2 Ph CH3 A-1327 CH2C(CH3)═CHCH3 Ph CH3 A-1328CH2CH═C(CH3)2 Ph CH3 A-1329 CH2CO2CH3 Ph CH3 A-1330 CH(CH3)CO2CH3 Ph CH3A-1331 C(CH3)2OC2CH3 Ph CH3 A-1332 CH2Ph Ph CH3 A-1333 CH2(3-CF3-Ph) PhCH3 A-1334 n-C3H7 Ph C2H5 A-1335 i-C3H7 Ph C2H5 A-1336 CH2CH═CH2 Ph C2H5A-1337 CH2C(CH3)═CH2 Ph C2H5 A-1338 CH2C(CH3)═CHCH3 Ph C2H5 A-1339CH2CH═C(CH3)2 Ph C2H5 A-1340 CH2CO2CH3 Ph C2H5 A-1341 CH(CH3)CO2CH3 PhC2H5 A-1342 C(CH3)2OC2CH3 Ph C2H5 A-1343 CH2Ph Ph C2H5 A-1344CH2(3-CF3-Ph) Ph C2H5 A-1345 n-C3H7 Ph i-C3H7 A-1346 i-C3H7 Ph i-C3H7A-1347 CH2CH═CH Ph i-C3H7 A-1348 CH2C(CH3)═CH2 Ph i-C3H7 A-1349CH2C(CH3)═CHCH3 Ph i-C3H7 A-1350 CH2CH═C(CH3)2 Ph i-C3H7 A-1351CH2CO2CH3 Ph i-C3H7 A-1352 CH(CH3)CO2CH3 Ph i-C3H7 A-1353 C(CH3)2OC2CH3Ph t-C3H7 A-1354 CH2Ph Ph i-C3H7 A-1355 CH2(3-CF3-Ph) Ph i-C3H7 A-1356CH2CH═CH 4-Cl-Ph CH3 A-1357 CH2Ph 4-Cl-Ph CH3 A-1358 CH2CH═CH2 4-CH3O-PhCH3 A-1359 CH2Ph 4-CH3O-Ph CH3 A-1360 CH2CH═CH 4-(4-Cl-Ph)O-Ph CH3A-1361 CH2Ph 4-(4-Cl-Ph)O-Ph CH3 A-1362 CH2CH═CH2 4-(4-CF3-Ph)O-Ph CH3A-1363 CH2Ph 4-(4-CF3-Ph)O-Ph CH3 A-1364 CH2CH═CH 4-CF3-Ph CH3 A-1365CH2CH═CH 4-CF3O-Ph CH3 A-1366 CH2CH═CH 4-CF3S-Ph CH3 A-1367 CH2CH═CH4-CF3CH2O-Ph CH3 A-1368 n-C3H7 2-thiazolyl H A-1369 i-C3H7 2-thiazolyl HA-1370 CH2CH═CH2 2-thiazolyl H A-1371 CH2C(CH3)═CH2 2-thiazolyl H A-1372CH2C(CH3)═CHCH3 2-thiazolyl H A-1373 CH2CH═C(CH3)2 2-thiazolyl H A-1374CH2CO2CH3 2-thiazolyl H A-1375 CH(CH3)CO2CH3 2-thiazolyl H A-1376C(CH3)2CO2CH3 2-thiazolyl H A-1377 CH2Ph 2-thiazolyl H A-1378CH2(3-CF3Ph) 2-thiazolyl H A-1379 n-C3H7 1,2,3-thiadiazol-2-yl H A-1380i-C3H7 1,2,3-thiadiazol-2-yl H A-1381 CH2CH═CH 1,2,3-thiadiazol-2-yl HA-1382 CH2C(CH3)═CH2 1,2,3-thiadiazol-2-yl H A-1383 CH2C(CH3)═CHCH31,2,3-thiadiazol-2-yl H A-1384 CH2CH═C(CH3)2 1,2,3-thiadiazoi-2-yl HA-1385 CH2CO2CH3 1,2,3-thiadiazol-2-yl H A-1386 CH(CH3)CO2CH31,2,3-thiadiazol-2-yl H A-1387 C(CH3)2OC2CH3 1,2,3-thiadiazol-2-yl HA-1388 CH2Ph 1,2,3-thiadiazol-2-yl H A-1389 CH2(3-CF3-Ph)1,2,3-thiadiazol-2-yl H A-1390 n-C3H7 NH2 CH3 A-1391 i-C3H7 NH2 CH3A-1392 CH2CH═CH2 NH2 CH3 A-1393 CH2C(CH3)═CH2 NH2 CH3 A-1394CH2C(CH3)═CHCH3 NH2 CH3 A-1395 CH2CH═C(CH3)2 NH2 CH3 A-1396 CH2Ph NH2CH3 A-1397 CH2(3-CF3-Ph) NH2 CH3 A-1398 n-C3H7 NH2 i-C3H7 A-1399 i-C3H7NH2 i-C3H7 A-1400 CH2CH═CH2 NH2 i-C3H7 A-1401 CH2C(CH3)═CH2 NH2 i-C3H7A-1402 CH2C(CH3)═CHCH3 NH2 i-C3H7 A-1403 CH2CH═C(CH3)2 NH2 i-C3H7 A-1404CH2Ph NH2 i-C3H7 A-1405 CH2(3-CF3-Ph) NH2 i-C3H7 A-1406 n-C3H7 NH2 CH2PhA-1407 i-C3H7 NH2 CH2Ph A-1408 CH2CH═CH2 NH2 CH2Ph A-1409 CH2C(CH3)═CH2NH2 CH2Ph A-1410 CH2C(CH3)═CHCH3 NH2 CH2Ph A-1411 CH2CH═C(CH3)2 NH2CH2Ph A-1412 CH2Ph NH2 CH2Ph A-1413 CH2(3-CF3-Ph) NH2 CH2Ph A-1414n-C3H7 NHCOCH3 CH3 A-1415 i-C3H7 NHCOCH3 CH3 A-1416 CH2CH═CH2 NHCOCH3CH3 A-1417 CH2C(CH3)═CH2 NHCOCH3 CH3 A-1418 CH2C(CH3)═CHCH3 NHCOCH3 CH3A-1419 CH2CH═C(CH3)2 NHCOCH3 CH3 A-1420 CH2Ph NHCOCH3 CH3 A-1421CH2(3-CF3-Ph) NHCOCH3 CH3 A-1422 n-C3H7 NHCOPh CH3 A-1423 i-C3H7 NHCOPhCH3 A-1424 CH2CH═CH2 NHCOPh CH3 A-1425 CH2C(CH3)═CH2 NHCOPh CH3 A-1426CH2C(CH3)═CHCH3 NHCOPh CH3 A-1427 CH2CH═C(CH3)2 NHCOPh CH3 A-1428 CH2PhNHCOPh CH3 A-1429 CH2(3-CF3-Ph) NHCOPh CH3 A-1430 CH3 N═C(CH3)2 PhA-1431 i-C3H7 N═C(CH3)2 Ph A-1432 CH2CH═CH2 N═C(CH3)2 Ph A-1433CH2C(CH3)═CH2 N═C(CH3)2 Ph A-1434 CH2CCH N═C(CH3)2 Ph A-1435 CH2PhN═C(CH3)2 Ph A-1436 CH3 3-CF3Ph H A-1437 CH2CH═CH2 3-CF3Ph H A-1438CH2Ph 3-CF3Ph H

Compounds of formula (Ib): (Ib)

Com- pound R¹ R² R³ B-1 CH3 CH3 H B-2 CH3 CH3 CH3 B-3 CH3 C2H5 H B-4 CH3C2H5 C2H5 B-5 CH3 n-C3H7 H B-6 CH3 i-C3H7 H B-7 CH3 i-C3H7 CH3 B-8 CH3i-C3H7 C2H5 B-9 CH3 n-C4H9 H B-10 CH3 n-C4H9 CH3 B-11 CH3 s-C4H9 H B-12CH3 i-C4H9 H B-13 CH3 t-C4H9 H B-14 CH3 n-C5H11 H B-15 CH3 n-C6H13 HB-16 CH3 CH2CH(C2H5)2 H B-17 CH3 CH(CH3)CH2CH2CH(CH3)CH3 H B-18 CH3CH2CH═CH2 H B-19 CH3 CH2CH═CH2 CH3 B-20 CH3 CH2C(CH3)═CH2 H B-21 CH3CH2C(CH3)═CHCH3 H B-22 CH3 CH2CH═C(CH3)2 H B-23 CH3 CH2CCl═CH2 H B-24CH3 CH2CH═CCl2 H B-25 CH3 CH2CH═CHCF3 H B-26 CH3 CH2CH═CHPh H B-27 CH3CH(CH3)CH═CH2 H B-28 CH3 CH2CCH H B-29 CH3 CH2CCCH3 H B-30 CH3 CH2CF3 HB-31 CH3 CH2OCH3 H B-32 CH3 CH2CH2OC2H5 H B-33 CH3 CH2CH2CH2OCH3 H B-34CH3 CH2CH2OPh H B-35 0H3 CH(OCH3)C2H5 H B-36 CH3 CH2CH(OCH3)2 H B-37 CH3CH2CH(OCH3)2 CH3 B-38 CH3 (CH2)5CN H B-39 CH3 CH2CH2CN H B-40 CH3CH2CH2CN CH3 B-41 CH3 cyclo-C3H5 H B-42 CH3 cyclo-C6H11 H B-43 CH3cycio-C6H11 CH3 B-44 CH3 CH2(cyclo-C3H5) H B-45 CH3 CH2(cyclo-C5H9) HB-46 CH3 CH2(cyclo-C6H11) H B-47 CH3 CH2Ph H B-48 CH3 CH2Ph CH3 B-49 CH3CH2Ph i- C3H7 B-50 CH3 CH2(2-Cl-Ph) H B-51 CH3 CH2(3-Cl-Ph) H B-52 CH3CH2(4-Cl-Ph) H B-53 CH3 CH2(2-CF3-Ph) H B-54 CH3 CH2(3-CF3-Ph) H B-55CH3 CH2(4-CF3-Ph) H B-56 CH3 CH2(2-F-Ph) H B-57 CH3 CH2(3-F-Ph) H B-58CH3 CH2(4-F-Ph) H B-59 CH3 CH2(3-Me-Ph) H B-60 CH3 CH2(4-Me-Ph) H B-61CH3 CH2(4-t-C4H9-Ph) H B-62 CH3 CH2(4-t-C4H9-Ph) CH3 B-63 CH3 CH(CH3)PhH B-64 CH3 CH(CH3)(2-Cl-Ph) H B-65 CH3 CH(CH3)(3-Cl-Ph) H B-66 CH3CH(CH3)(4-Br-Ph) H B-67 CH3 CH(CH3)(4-Br-Ph) H B-68 CH3 CH2(2-thienyl) HB-69 CH3 CH2(2-pyridyl) H B-70 CH3 CH2CH2Ph H B-71 CH3 CH2CH2CH2CH2 B-72CH3 CH2CH2CH2CH2CH2 B-73 CH3 CH2CH2CH(CO2C2H5)CH2CH2 B-74 CH3 O(i-C3H7)B-75 CH3 OCH2C(CH3)CH2 H B-76 CH3 O(2-tetrahydropyranyl) H B-77 CH3OCH2(3,4-Cl2-Ph) H B-78 CH3 OCH2(2,4-Cl2-Ph) H B-79 CH3 OCH2(3-CF3-Ph) HB-80 CH3 OCH2(4-F-2-OCF3-Ph) H B-81 CH3 OCH2(2,5-(CF3)2-Ph) H B-82 CH3(CH2)2N(CH3)2 H B-83 CH3 (CH2)3N(CH3)2 H B-84 CH3 (CH2)3(1-imidazolyl) HB-85 CH3 CH2(1-C2H5-2-pyrrolidinyl) H B-86 CH3 NH(2-CF3-Ph) H B-87 CH3NH(4-Cl-Ph) H B-88 CH3 N(CH3)2 H B-89 C2H5 CH3 K B-90 C2H5 CH3 CH3 B-91C2H5 C2H5 H B-92 C2H5 C2H5 C2H5 B-93 C2H5 n-C3H7 H B-94 C2H5 i-C3H7 HB-95 C2H5 n-C4H9 H B-96 C2H5 s-C4H9 H B-97 C2H5 i-C4H9 K B-98 C2H5t-C4H9 K B-99 C2H5 n-C5H11 H B-100 C2H5 n-C6H13 H B-101 C2H5CH2CH(C2H5)2 H B-102 C2H5 CH(CH3)CH2CH2CH(CH3)CH3 H B-103 C2H5 CH2CH═CH2H B-104 C2H5 CH2CH═CH2 CH3 B-105 C2H5 CH2C(CH3)═CH2 H B-106 C2H5CH2C(CH3)═CHCH3 H B-107 C2H5 CH2CH═C(CH3)2 H B-108 C2H5 CH2CCl═CH2 HB-109 C2H5 CH2CH═CCl2 H B-110 C2H5 CH2CH═CHCF3 H B-111 C2H5 CH2CH═CHPh HB-112 C2H5 CH(CH3)CH═CH2 H B-113 C2H5 CH2CCH H B-114 C2H5 CH2CCH CH3B-115 C2H5 CH2CCCH3 H B-116 C2H5 CH2CF3 H B-117 C2H5 CH2CH2OCH3 H B-118C2H5 CH2CH2OC2H5 H B-119 C2H5 CH2CH2CH2OCH3 H B-120 C2H5 CH2CH2CH2OC2H5H B-121 C2H5 CH(OCH3)C2H5 H B-122 C2H5 CH2CH(OCH3)2 H B-123 C2H5CH2CH(OCH3)2 CH3 B-124 C2H5 (CH2)5CN H B-125 C2H5 cyclo-C3H5 H B-126C2H5 cyclo-C6H11 H B-127 C2H5 CH2(cyclo-C3H5) H B-128 C2H5CH2(cyclo-C5H9) H B-129 C2H5 CH2(cyclo-C6H11) H B-130 C2H5 CH2Ph H B-131C2H5 CH2(2-Cl-Ph) H B-132 C2H5 CH2(3-Cl-Ph) H B-133 C2H5 CH2(4-Cl-Ph) HB-134 C2H5 CH2(2-CF3-Ph) H B-135 C2H5 CH2(3-CF3-Ph) H B-136 C2H5CH2(4-CF3-Ph) H B-137 C2H5 CH2(2-F-Ph) H B-138 C2H5 CH2(3-F-Ph) H B-139C2H5 CH2(4-F-Ph) H B-140 C2H5 CH2(3-Me-Ph) H B-141 C2H5 CH2(4-Me-Ph) HB-142 C2H5 CH(CH3)Ph H B-143 C2H5 CH(CH3)(2-Cl-Ph) H B-144 C2H5CH(CH3)(3-Cl-Ph) H B-145 C2H5 CH(CH3)(4-Cl-Ph) H B-146 C2H5CH(CH3)(2-CF3-Ph) H B-147 C2H5 CH(CH3)(3-CF3-Ph) H B-148 C2H5CH(CH3)(4-CF3-Ph) H B-149 C2H5 CH2CH2Ph H B-150 C2H5 CH2(2-thienyl) HB-151 C2H5 CH2(2-furanyl) H B-152 C2H5 OCH2C(CH3)═CH2 H B-153 C2H5O(2-tetrahydropyranyl) H B-154 C2H5 OCH2(3,4-Cl2-Ph) H B-155 C2H5OCH2(2,4-Cl2-Ph) H B-156 C2H5 OCH2(3-CF3-Ph) H B-157 C2H5OCH2(4-F-2-CF3-Ph) H B-158 C2H5 OCH2(2,5-(CF3)2-Ph) H B-159 C2H5(CH2)2N(CH3)2 H B-160 C2H5 (CH2)3N(CH3)2 H B-161 C2H5(CH2)3(1-imidazolyl) H B-162 C2H5 CH2(1-C2H5-2-pyrrolidynyl) H B-163C2H5 NH(2-CF3-Ph) H B-164 C2H5 NH(4-Cl-Ph) H B-I65 C2H5 N(CH3)2 H B-166i-C3H7 CH3 H B-167 i-C3H7 CH3 CH3 B-168 i-03H7 C2H5 H B-169 i-03H7 C2H5C2H5 B-170 i-C3H7 n-C3H7 H B-171 i-C3H7 i-C3H7 H B-172 i-C3H7 n-C4H9 HB-173 i-C3H7 s-C4H9 H B-174 i-C3H7 i-C4H9 H B-175 i-C3H7 t-C4H9 H B-176i-C3H7 n-C5H11 H B-177 i-C3H7 n-C6H13 H B-178 i-C3H7 CH2CH(C2H5)2 HB-179 i-C3H7 CH(CH3)CH2CH2CH(CH3)CH3 H B-180 i-C3H7 CH2CH═CH2 H B-181i-C3H7 CH2CHCH2 CH3 B-182 i-C3H7 CH2C(CH3)═CH2 H B-183 i-C3H7CH2C(CH3)═CHCH3 H B-184 i-C3H7 CH2CH═C(CH3)2 H B-185 i-C3H7 CH2CCl═CH2 HB-186 i-C3H7 CH2CH═OCl2 H B-187 i-03H7 CH2CH═CHCF3 H B-188 i-C3H7CH2CH═CHPh H B-189 i-C3H7 CH(CH3)CH═CH2 H B-190 i-C3H7 CH2CCH H B-191i-C3H7 CH2CCH CH3 B-192 i-C3HJ CH2CCCH3 H B-193 i-C3H7 CH2CF3 H B-194i-C3H7 CH2CH2OCH3 H B-195 i-C3H7 CH2CH2OC2H5 H B-196 i-C3H7CH2CH2CH2OCH3 H B-197 i-C3H7 CH2CH2CH2OC2H5 H B-198 i-C3H7 CH(OCH3)C2H5H B-199 i-C3H7 CH2CH(OCH3)2 H B-200 i-C3H7 CH2CH(OCH3)2 CH3 B-201 i-C3H7(CH2)5CN H B-202 i-C3H7 CH2CH2CN H B-203 i-C3H7 CH2CH2CN CH3 B-204i-C3H7 CH2CH2CN C2H5 B-205 i-C3H7 cyclo-C3H5 H B-206 i-C3H7 cycto-C6H11H B-207 i-C3H7 CH2(cyclo-C3H5) H B-208 i-C3H7 CH2(cyclo-C5H9) H B-209i-C3H7 CH2(cyclo-C6H11) H B-210 i-C3H7 CH2Ph H B-211 i-C3H7 CH2(2-Cl-Ph)H B-212 i-C3H7 CH2(3-Cl-Ph) H B-213 i-C3H7 CH2(4-Cl-Ph) H B-214 i-C3H7CH2(2-CF3-Ph) H B-215 i-C3H7 CH2(3-CF3-Ph) H B-216 i-C3H7 CH2(4-CF3-Ph)H B-217 i-C3H7 CH2(2-F-Ph) H B-218 i-C3H7 CH2(3-F-Ph) H B-219 i-C3H7CH2(4-F-Ph) H B-220 i-C3H7 CH2(3-Me-Ph) H B-221 i-C3H7 CH2(4-Me-Ph) HB-222 i-C3H7 CH(CH3)Ph H B-223 i-C3H7 CH(CH3)(2-Cl-Ph) H B-224 i-C3H7CH(CH3)(3-Cl-Ph) H B-225 i-C3H7 CH(CH3)(4-Cl-Ph) H B-226 i-C3H7CH(CH3)(2-CF3-Ph) H B-227 i-C3H7 CH(CH3)(3-CF3-Ph) H B-228 i-C3H7CH(CH3)(4-CF3-Ph) H B-229 i-C3H7 CH2CH2Ph H B-230 i-C3H7 CH2(2-thienyl)H B-231 i-C3H7 CH2(2-furanyl) H B-232 i-C3H7 OCH2C(CH3)═CH2 H B-233i-C3H7 O(2-tetrahydropyranyl) H B-234 i-C3H7 OCH2(3,4-Cl2-Ph) H B-235i-C3H7 OCH2(2,4-Cl2-Ph) H B-236 i-C3H7 OCH2(3-CF3-Ph) H B-237 i-C3H7OCH2(4-F-2-CF3-Ph) H B-238 i-C3H7 OCH2((CF3)2-Ph) H B-239 i-C3H7(CH2)2N(CH3)2 H B-240 i-C3H7 (CH2)3N(CH3)2 H B-241 i-C3H7(CH2)3(1-imidazolyl) H B-242 i-C3H7 CH2(1-C2H5-2-pyrrolidinyl) H B-243i-C3H7 NH(2-CF3-Ph) H B-244 i-C3H7 NH(4-Cl-Ph) H B-245 i-C3H7 N(CH3)2 HB-246 CH3 NH(3-CF3-Ph) H B-247 (CH2)3SCH3 CH2CH2N(CH3)2 H B-248(CH2)3SCH3 CH2CCH H B-249 CH3 OCH2(6-F-benzo-1,3-dioxan- H 4-yl) B-250CH3 OCH2(4-F-2-CF3-Ph) H B-251 CH3 OCH2(2-OCF3-Ph) H B-252 CH3CH(CH3)(4-Cl-Ph) H B-253 CH3 CH2CCH CH3 B-254 CH3CH2(1,3-benzodioxofan-5-yl) H B-255 CH3 CH2CH(C2H5)2 H B-256 CH3CH2(2-furyl) H

TABLE 3 Compounds of formula (Ic): (Ic)

Compound R⁴ R¹ C-1 CH2OH═CH2 CH3 C-2 CH2C(CH3)═CH2 CH3 C-3CH2C(CH3)═CHCH3 CH3 C-4 CH2CH═C(CH3)2 CH3 C-5 CH2CCl═CH2 CH3 C-6CH2OH═CCl2 CH3 C-7 CH2CH═CHCF3 CH3 C-8 CH2CH═CHPh CH3 C-9 CH(CH3)CH═CH2CH3 C-10 CH2CCH CH3 C-11 CH2CCCH3 CH3 C-12 CH2CF3 CH3 C-13 CH2CH2OCH3CH3 C-14 CH2CH2OC2H5 CH3 C-15 CH2CH2CH2OCH3 CH3 C-16 CH2CH2CH2OC2H5 CH3C-17 CH2OH(OCH3)2 CH3 C-18 CH2CN CH3 C-19 CH2(cyclo-C3H5) CH3 C-20CH2(cyclo-C5H9) CH3 C-21 CH2(cyclo-C6H11) CH3 C-22 CH2Ph CH3 C-23CH2(2-Cl-Ph) CH3 C-24 CH2(3-Cl-Ph) CH3 C-25 CH2(4-Cl-Ph) CH3 C-26CH2(2-CF3-Ph) CH3 C-27 CH2(3-CF3-Ph) CH3 C-28 CH2(4-CF3-Ph) CH3 C-29CH2(2-F-Ph) CH3 C-30 CH2(3-F-Ph) CH3 C-31 CH2(4-F-Ph) CH3 C-32CH2(2-OMe-Ph) CH3 C-33 CH2(3-OMe-Ph) CH3 C-34 CH2(4-OMe-Ph) CH3 C-35CH(CH3)Ph CH3 C-36 CH(CH3)(2-Cl-Ph) CH3 C-37 CH(CH3)(3-Cl-Ph) CH3 C-38CH(CH3)(4-Cl-Ph) CH3 C-39 CH(CH3)(2-CF3-Ph) CH3 C-40 CH(CH3)(3-CF3-Ph)CH3 C-41 CH(CH3)(4-CF3-Ph) CH3 C-42 CH2CH2Ph CH3 C-43 CH2CH═CH2 02H5C-44 CH2C(CH3)═CH2 C2H5 C-45 CH2C(CH3)═CHCH3 C2H5 C-46 CH2CH═C(CH3)2C2H5 C-47 CH2CCl═CH2 C2H5 C-48 CH2CH═CCl2 C2H5 C-49 CH2CH═CHCF3 C2H5C-50 CH2CH═CHPh C2H5 C-51 CH(CH3)CH═CH2 C2H5 C-52 CH2CCH C2H5 C-53CH2CCCH3 C2H5 C-54 CH2CF3 C2H5 C-55 CH2CH2OCH3 C2H5 C-56 CH2CH2OC2H5C2H5 C-57 CH2CH2CH2OCH3 C2H5 C-58 CH2CH2CH2OC2H5 C2H5 C-59 CH2OH(OCH3)2C2H5 C-60 CH2CN C2H5 C-61 CH2(cyclo-C3H5) C2H5 C-62 CH2(cyclo-C5H9) C2H5C-63 CH2(cycto-C6H11) C2H5 C-64 CH2Ph C2H5 C-65 CH2(2-Cl-Ph) C2H5 C-66CH2(3-Cl-Ph) C2H5 C-67 CH2(4-Cl-Ph) C2H5 C-68 CH2(2-CF3-Ph) C2H5 C-69CH2(3-CF3-Ph) C2H5 C-70 CH2(4-CF3-Ph) C2H5 C-71 CH2(2-F-Ph) C2H5 C-72CH2(3-F-Ph) C2H5 C-73 CH2(4-F-Ph) C2H5 C-74 CH2(2-OMe-Ph) C2H5 C-75CH2(3-OMe-Ph) C2H5 C-76 CH2(4-OMe-Ph) C2H5 C-77 CH(CH3)Ph C2H5 C-78CH(CH3)(2-Cl-Ph) C2H5 C-79 CH(CH3)(3-Cl-Ph) C2H5 C-80 CH(CH3)(4-Cl-Ph)C2H5 C-81 CH(CH3)(2-CF3-Ph) C2H5 C-82 CH(CH3)(3-CF3-Ph) C2H5 C-83CH(CH3)(4-CF3-Ph) C2H5 C-84 CH2OH2Ph C2H5 C-85 CH2CH═CH2 n-C3H7 C-86CH2C(CH3)═CH2 n-C3H7 C-87 CH2C(CH3)═CHCH3 n-C3H7 C-88 CH2CH═C(CH3)2n-C3H7 C-89 CH2CCl═CH2 n-C3H7 C-90 CH2CH═CCl2 n-C3H7 C-91 CH2CH═CHCF3n-C3H7 C-92 CH2CH═CHPh n-C3H7 C-93 CH(CH3)CH═CH2 n-C3H7 C-94 CH2CCHn-C3H7 C-95 CH2CCCH3 n-C3H7 C-96 CH2CF3 n-C3H7 C-97 CH2CH2OCH3 n-C3H7C-98 CH2CH2OC2H5 n-C3H7 C-99 CH2CH2CH2OCH3 n-C3H7 C-100 CH2CH2CH2OC2H5n-C3H7 C-101 CH2CH(OCH3)2 n-C3H7 C-102 CH2CN n-C3H7 C-103CH2(cyclo-C3H5) n-C3H7 C-104 CH2(cyclo-C5H9) n-C3H7 C-105CH2(cyclo-C6H11) n-C3H7 C-106 CH2Ph n-C3H7 C-107 CH2(2-Cl-Ph) n-C3H7C-108 CH2(3-Cl-Ph) n-C3H7 C-109 CH2(4-Cl-Ph) n-C3H7 C-110 CH2(2-CF3-Ph)n-C3H7 C-111 CH2(3-CF3-Ph) n-C3H7 C-112 CH2(4-CF3-Ph) n-C3H7 C-113CH2(2-F-Ph) n-C3H7 C-114 CH2(3-F-Ph) n-C3H7 C-115 CH2(4-F-Ph) n-C3H7C-116 CH2(2-OMe-Ph) n-C3H7 C-117 CH2(3-OMe-Ph) n-C3H7 C-118CH2(4-OMe-Ph) n-C3H7 C-119 CH(CH3)Ph n-C3H7 C-120 CH(CH3)(2-Cl-Ph)n-C3H7 C-121 CH(CH3)(3-Cl-Ph) n-C3H7 C-122 CH(CH3)(4-Cl-Ph) n-C3H7 C-123CH(CH3)(2-CF3-Ph) n-C3H7 C-124 CH(CH3)(3-CF3-Ph) n-C3H7 C-125CH(CH3)(4-CF3-Ph) n-C3H7 C-126 CH2OH2Ph n-C3H7 C-127 CH2CH═CH2 i-C3H7C-128 CH2C(CH3)═CH2 i-C3H7 C-129 CH2C(CH3)═CHCH3 i-C3H7 C-130CH2CH═C(CH3)2 i-C3H7 C-131 CH2CCl═CH2 i-C3H7 C-132 CH2CH═CCl2 i-C3H7C-133 CH2CH═CHCF3 i-C3H7 C-134 CH2CH═CHPh i-C3H7 C-135 CH(CH3)CH═CH2i-C3H7 C-136 CH2CCH i-C3H7 C-137 CH2CCCH3 i-C3H7 C-138 CH2CF3 i-C3H7C-139 CH2CH2OCH3 i-C3H7 C-140 CH2CH2OC2H5 i-C3H7 C-141 CH2CH2CH2OCH3i-C3H7 C-142 CH2CH2OH2OC2H5 i-C3H7 C-143 CH2CH(OCH3)2 i-C3H7 C-144 CH2CNi-C3H7 C-145 CH2(cyclo-C3H5) i-C3H7 C-146 CH2(cyclo-C5H9) i-C3H7 C-147CH2(cyclo-C6H11) i-C3H7 C-148 CH2Ph i-C3H7 C-149 CH2(2-Cl-Ph) i-C3H7C-150 CH2(3-Cl-Ph) i-C3H7 C-151 CH2(4-Cl-Ph) i-C3H7 C-152 CH2(2-CF3-Ph)i-C3H7 C-153 CH2(3-CF3-Ph) i-C3H7 C-154 CH2(4-CF3-Ph) i-C3H7 C-155CH2(2-F-Ph) i-C3H7 C-156 CH2(3-F-Ph) i-C3H7 C-157 CH2(4-F-Ph) i-C3H7C-158 CH2(2-OMe-Ph) i-C3H7 C-159 CH2(3-OMe-Ph) i-C3H7 C-160CH2(4-OMe-Ph) i-C3H7 C-161 CH(CH3)Ph i-C3H7 C-162 CH(CH3)(2-Cl-Ph)i-C3H7 C-163 CH(CH3)(3-Cl-Ph) i-C3H7 C-164 CH(CH3)(4-Cl-Ph) i-C3H7 C-165CH(CH3)(2-CF3-Ph) i-C3H7 C-166 CH(CH3)(3-CF3-Ph) i-C3H7 C-167CH(CH3)(4-CF3-Ph) i-C3H7 C-168 CH2CH2Ph i-C3H7 C-169 CH2CH═CH2 n-C4H9C-170 CH2C(CH3)═CH2 n-C4H9 C-171 CH2C(CH3)═CHCH3 n-C4H9 C-172CH2CH═C(CH3)2 n-C4H9 C-173 CH2CCl═CH2 n-C4H9 C-174 CH2CH═CCl2 n-C4H9C-175 CH2CH═CHCF3 n-C4H9 C-176 CH2CH═CHPh n-C4H9 C-177 CH(CH3)CH═CH2n-C4H9 C-178 CH2CCH n-C4H9 C-179 CH2CCCH3 n-C4H9 C-180 CH2CF3 n-C4H9C-181 CH2CH2OCH3 n-C4H9 C-182 CH2CH2OC2H5 n-C4H9 C-183 CH2CH2CH2OCH3n-C4H9 C-184 CH2CH2CH2OC2H5 n-C4H9 C-185 CH2CH(OCH3)2 n-C4H9 C-186 CH2CNn-C4H9 C-187 CH2(cyclo-C3H5) n-C4H9 C-188 CH2(cyclo-C5H9) n-C4H9 C-189CH2(cyclo-C6H11) n-C4H9 C-190 CH2Ph n-C4H9 C-191 CH2(2-Cl-Ph) n-C4H9C-192 CH2(3-Cl-Ph) n-C4H9 C-193 CH2(4-Cl-Ph) n-C4H9 C-194 CH2(2-CF3-Ph)n-C4H9 C-195 CH2(3-CF3-Ph) n-C4H9 C-196 CH2(4-CF3-Ph) n-C4H9 C-197CH2(2-F-Ph) n-C4H9 C-198 CH2(3-F-Ph) n-C4H9 C-199 CH2(4-F-Ph) n-C4H9C-200 CH2(2-OMe-Ph) n-C4H9 C-201 CH2(3-OMe-Ph) n-C4H9 C-202CH2(4-OMe-Ph) n-C4H9 C-203 CH(CH3)Ph n-C4H9 C-204 CH(CH3)(2-Cl-Ph)n-C4H9 C-205 CH(CH3)(3-Cl-Ph) n-C4H9 C-206 CH(CH3)(4-Cl-Ph) n-C4H9 C-207CH(CH3)(2-CF3-Ph) n-C4H9 C-208 CH(CH3)(3-CF3-Ph) n-C4H9 C-209CH(CH3)(4-CF3-Ph) n-C4H9 C-210 CH2CH2Ph n-C4H9 C-211 CH2CH═CH2 i-C4H9C-212 CH2C(CH3)═CH2 i-C4H9 C-213 CH2C(CH3)═CHCH3 i-C4H9 C-214CH2CH═C(CH3)2 1-C4H9 C-215 CH2CCl═CH2 i-C4H9 C-216 CH2CH═CCl2 i-C4H9C-217 CH2CH═CHCF3 i-C4H9 C-218 CH2CH═CHPh i-C4H9 C-219 CH(CH3)OH═CH2i-C4H9 C-220 CH2CCH i-C4H9 C-221 CH2CCCH3 i-C4H9 C-222 CH2CF3 i-C4H9C-223 CH2CH2OCH3 i-C4H9 C-224 CH2CH2OC2H5 i-C4H9 C-225 CH2OH2CH2OCH3i-C4H9 C-226 CH2CH2OH2OC2H5 i-C4H9 C-227 CH2CH(OCH3)2 i-C4H9 C-228 CH2CNi-C4H9 C-229 CH2(cyclo-C3H5) i-C4H9 C-230 CH2(cyclo-C5H9) i-C4H9 C-231CH2(cyclo-C6H11) i-C4H9 C-232 CH2Ph i-C4H9 C-233 CH2(2-Cl-Ph) i-C4H9C-234 CH2(3-Cl-Ph) i-C4H9 C-235 CH2(4-Cl-Ph) i-C4H9 C-236 CH2(2-CF3-Ph)i-C4H9 C-237 CH2(3-CF3-Ph) i-C4H9 C-238 CH2(4-CF3-Ph) i-C4H9 C-239CH2(2-F-Ph) i-C4H9 C-240 CH2(3-F-Ph) i-C4H9 C-241 CH2(4-F-Ph) i-C4H9C-242 CH2(2-OMe-Ph) i-C4H9 C-243 CH2(3-OMe-Ph) i-C4H9 C-244CH2(4-OMe-Ph) i-C4H9 C-245 CH(CH3)Ph i-C4H9 C-246 CH(CH3)(2-Cl-Ph)i-C4H9 C-247 CH(CH3)(3-Cl-Ph) i-C4H9 C-248 CH(CH3)(4-Cl-Ph) i-C4H9 C-249CH(CH3)(2-CF3-Ph) i-C4H9 C-250 CH(CH3)(3-CF3-Ph) i-C4H9 C-251CH(CH3)(4-CF3-Ph) i-C4H9 C-252 CH2CH2Ph i-C4H9 C-253 CH2CH═CH2 sec-C4H9C-254 CH2C(CH3)═CH2 sec-C4H9 C-255 CH2C(CH3)═CHCH3 sec-C4H9 C-256CH2CH═C(CH3)2 sec-C4H9 C-257 CH2CCl═CH2 sec-C4H9 C-258 CH2CH═CCl2sec-C4H9 C-259 CH2CH═CHCF3 sec-C4H9 C-260 CH2CH═CHPh sec-C4H9 C-261CH(CH3)CH═CH2 sec-C4H9 C-262 CH2CCH sec-C4H9 C-263 CH2CCCH3 sec-C4H9C-264 CH2CF3 sec-C4H9 C-265 CH2CH2OCH3 sec-C4H9 C-266 CH2CH2OC2H5sec-C4H9 C-267 CH2CH2CH2OCH3 sec-C4H9 C-268 CH2CH2CH2OC2H5 sec-C4H9C-269 CH2CH(OCH3)2 sec-C4H9 C-270 CH2CN sec-C4H9 C-271 CH2(cyclo-C3H5)sec-C4H9 C-272 CH2(cyclo-C5H9) sec-C4H9 C-273 CH2(cyclo-C6H11) sec-C4H9C-274 CH2Ph sec-C4H9 C-275 CH2(2-Cl-Ph) sec-C4H9 C-276 CH2(3-Cl-Ph)sec-C4H9 C-277 CH2(4-Cl-Ph) sec-C4H9 C-278 CH2(2-CF3-Ph) sec-C4H9 C-279CH2(3-CF3-Ph) sec-C4H9 C-280 CH2(4-CF3-Ph) sec-C4H9 C-281 CH2(2-F-Ph)sec-C4H9 C-282 CH2(3-F-Ph) sec-C4H9 C-283 CH2(4-F-Ph) sec-C4H9 C-284CH2(2-OMe-Ph) sec-C4H9 C-285 CH2(3-OMe-Ph) sec-C4H9 C-286 CH2(4-OMe-Ph)sec-C4H9 C-287 CH(CH3)Ph sec-C4H9 C-288 CH(CH3)(2-Cl-Ph) sec-C4H9 C-289CH(CH3)(3-Cl-Ph) sec-C4H9 C-290 CH(CH3)(4-Cl-Ph) sec-C4H9 C-291CH(CH3)(2-CF3-Ph) sec-C4H9 C-292 CH(CH3)(3-CF3-Ph) sec-C4H9 C-293CH(CH3)(4-CF3-Ph) sec-C4H9 C-294 CH2CH2Ph sec-C4H9 C-295 CH2CH═CH2t-C4H9 C-296 CH2C(CH3)═CH2 t-C4H9 C-297 CH2C(CH3)═CHCH3 t-C4H9 C-298CH2CH═C(CH3)2 t-C4H9 C-299 CH2CCl═CH2 t-C4H9 C-300 CH2CH═CCl2 t-C4H9C-301 CH2CH═CHCF3 t-C4H9 C-302 CH2CH═CHPh t-C4H9 C-303 CH(CH3)CH═CH2t-C4H9 C-304 CH2CCH t-C4H9 C-305 CH2CCCH3 t-C4H9 C-306 CH2CF3 t-C4H9C-307 CH2CH2OCH3 t-C4H9 C-308 CH2CH2OC2H5 t-C4H9 C-309 CH2CH2CH2OCH3t-C4H9 C-310 CH2CH2CH2OC2H5 t-C4H9 C-311 CH2CH(OCH3)2 t-C4H9 C-312 CH2CNt-C4H9 C-313 CH2(cyclo-C3H5) t-C4H9 C-314 CH2(cyclo-C5H9) t-C4H9 C-315CH2(cyclo-C6H11) t-C4H9 C-316 CH2Ph t-C4H9 C-317 CH2(2-Cl-Ph) t-C4H9C-318 CH2(3-Cl-Ph) t-C4H9 C-319 CH2(4-Cl-Ph) t-C4H9 C-320 CH2(2-CF3-Ph)t-C4H9 C-321 CH2(3-CF3-Ph) t-C4H9 C-322 CH2(4-CF3-Ph) t-C4H9 C-323CH2(2-F-Ph) t-C4H9 C-324 CH2(3-F-Ph) t-C4H9 C-325 CH2(4-F-Ph) t-C4H9C-326 CH2(2-OMe-Ph) t-C4H9 C-327 CH2(3-OMe-Ph) t-C4H9 C-328CH2(4-OMe-Ph) t-C4H9 C-329 CH(CH3)Ph t-C4H9 C-330 CH(CH3)(2-Cl-Ph)t-C4H9 C-331 CH(CH3)(3-Cl-Ph) t-C4H9 C-332 CH(CH3)(4-Cl-Ph) t-C4H9 C-333CH(CH3)(2-CF3-Ph) t-C4H9 C-334 CH(CH3)(3-CF3-Ph) t-C4H9 C-335CH(CH3)(4-CF3-Ph) t-C4H9 C-336 CH2CH2Ph t-C4H9 C-337 CH2CH═CH2 n-C5H11C-338 CH2C(CH3)═CH2 n-C5H11 C-339 CH2C(CH3)═CHCH3 n-C5H11 C-340CH2CH═C(CH3)2 n-C5H11 C-341 CH2CCl═CH2 n-C5H11 C-342 CH2CH═CCl2 n-C5H11C-343 CH2CH═CHCF3 n-C5H11 C-344 CH2CH═CHPh n-C5H11 C-345 CH(CH3)CH═CH2n-C5H11 C-346 CH2CCH n-C5H11 C-347 CH2CCCH3 n-C5H11 C-348 CH2CF3 n-C5H11C-349 CH2CH2OCH3 n-C5H11 C-350 CH2CH2OC2H5 n-C5H11 C-351 CH2CH2CH2OCH3n-C5H11 C-352 CH2CH2CH2OC2H5 n-C5H11 C-353 CH2CH(OCH3)2 n-C5H11 C-354CH2CN n-C5H11 C-355 CH2(cyclo-C3H5) n-C5H11 C-356 CH2(cyclo-C5H9)n-C5H11 C-357 CH2(cyclo-C6H11) n-C5H11 C-358 CH2Ph n-C5H11 C-359CH2(2-Cl-Ph) n-C5H11 C-360 CH2(3-Cl-Ph) n-C5H11 C-361 CH2(4-Cl-Ph)n-C5H11 C-362 CH2(2-CF3-Ph) n-C5H11 C-363 CH2(3-CF3-Ph) n-C5H11 C-364CH2(4-CF3-Ph) n-C5H11 C-365 CH2(2-F-Ph) n-C5H11 C-366 CH2(3-F-Ph)n-C5H11 C-367 CH2(4-F-Ph) n-C5H11 C-368 CH2(2-OMe-Ph) n-C5H11 C-369CH2(3-OMe-Ph) n-C5H11 C-370 CH2(4-OMe-Ph) n-C5H11 C-371 CH(CH3)Phn-C5H11 C-372 CH(CH3)(2-Cl-Ph) n-C5H11 C-373 CH(CH3)(3-Cl-Ph) n-C5H11C-374 CH(CH3)(4-Cl-Ph) n-C5H11 C-375 CH(CH3)(2-CF3-Ph) n-C5H11 C-376CH(CH3)(3-CF3-Ph) n-C5H11 C-377 CH(CH3)(4-CF3-Ph) n-C5H11 C-378 CH2CH2Phn-C5H11 C-379 CH2CH═CH2 n-C6H13 C-380 CH2C(CH3)═CH2 n-C6H13 C-381CH2C(CH3)═CHCH3 n-C6H13 C-382 CH2CH═C(CH3)2 n-C6H13 C-383 CH2CCl═CH2n-C6H13 C-384 CH2CH═CCl2 n-C6H13 C-385 CH2CH═CHCF3 n-C6H13 C-386CH2CH═CHPh n-C6H13 C-387 CH(CH3)CH═CH2 n-C6H13 C-388 CH2CCH n-C6H13C-389 CH2CCCH3 n-C6H13 C-390 CH2CF3 n-C6H13 C-391 CH2CH2OCH3 n-C6H13C-392 CH2CH2OC2H5 n-C6H13 C-393 CH2CH2CH2OCH3 n-C6H13 C-394CH2CH2CH2OC2H5 n-C6H13 C-395 CH2CH(OCH3)2 n-C6H13 C-396 CH2CN n-C6H13C-397 CH2(cyclo-C3H5) n-C6H13 C-398 CH2(cyclo-C5H9) n-C6H13 C-399CH2(cyclo-C6H11) n-C6H13 C-400 CH2Ph n-C6H13 C-401 CH2(2-Cl-Ph) n-C6H13C-402 CH2(3-Cl-Ph) n-C6H13 C-403 CH2(4-Cl-Ph) n-C6H13 C-404CH2(2-CF3-Ph) n-C6H13 C-405 CH2(3-CF3-Ph) n-C6H13 C-406 CH2(4-CF3-Ph)n-C6H13 C-407 CH2(2-F-Ph) n-C6H13 C-408 CH2(3-F-Ph) n-C6H13 C-409CH2(4-F-Ph) n-C6H13 C-410 CH2(2-OMe-Ph) n-C6H13 C-411 CH2(3-OMe-Ph)n-C6H13 C-412 CH2(4-OMe-Ph) n-C6H13 C-413 CH(CH3)Ph n-C6H13 C-414CH(CH3)(2-Cl-Ph) n-C6H13 C-415 CH(CH3)(3-Cl-Ph) n-C6H13 C-416CH(CH3)(4-Cl-Ph) n-C6H13 C-417 CH(CH3)(2-CF3-Ph) n-C6H13 C-418CH(CH3)(3-CF3-Ph) n-C6H13 C-419 CH(CH3)(4-CF3-Ph) n-C6H13 C-420 CH2CH2Phn-C6H13 C-421 CH2CH═CH2 cyclo-C5H9 C-422 CH2C(CH3)═CH2 cyclo-C5H9 C-423CH2C(CH3)═CHCH3 cyclo-C5H9 C-424 CH2CH═C(CH3)2 cyclo-C5H9 C-425CH2CCl═CH2 cyclo-C5H9 C-426 CH2CH═CCl2 cyclo-C5H9 C-427 CH2CH═CHCF3cyclo-C5H9 C-428 CH2CH═CHPh cyclo-C5H9 C-429 CH(CH3)CH═CH2 cyclo-C5H9C-430 CH2CCH cyclo-C5H9 C-431 CH2CCCH3 cyclo-C5H9 C-432 CH2CF3cyclo-C5H9 C-433 CH2CH2OCH3 cyclo-C5H9 C-434 CH2CH2OC2H5 cyclo-C5H9C-435 CH2CH2CH2OCH3 cyclo-C5H9 C-436 CH2CH2CH2OC2H5 cyclo-C5H9 C-437CH2CH(OCH3)2 cyclo-C5H9 C-438 CH2CN cyclo-C5H9 C-439 CH2(cyclo-C3H5)cyclo-C5H9 C-440 CH2(cyclo-C5H9) cyclo-C5H9 C-441 CH2(cyclo-C6H11)cyclo-C5H9 C-442 CH2Ph cyclo-C5H9 C-443 CH2(2-Cl-Ph) cyclo-C5H9 C-444CH2(3-Cl-Ph) cyclo-C5H9 C-445 CH2(4-Cl-Ph) cyclo-C5H9 C-446CH2(2-CF3-Ph) cyclo-C5H9 C-447 CH2(3-CF3-Ph) cyclo-C5H9 C-448CH2(4-CF3-Ph) cyclo-C5H9 C-449 CH2(2-F-Ph) cyclo-C5H9 C-450 CH2(3-F-Ph)cyclo-C5H9 C-451 CH2(4-F-Ph) cyclo-C5H9 C-452 CH2(2-OMe-Ph) cyclo-C5H9C-453 CH2(3-OMe-Ph) cyclo-C5H9 C-454 CH2(4-OMe-Ph) cyclo-C5H9 C-455CH(CH3)Ph cyclo-C5H9 C-456 CH(CH3)(2-Cl-Ph) cyclo-C5H9 C-457CH(CH3)(3-Cl-Ph) cyclo-C5H9 C-458 CH(CH3)(4-Cl-Ph) cyclo-C5H9 C-459CH(CH3)(2-CF3-Ph) cyclo-C5H9 C-460 CH(CH3)(3-CF3-Ph) cyclo-C5H9 C-461CH(CH3)(4-CF3-Ph) cyclo-C5H9 C-462 CH2CH2Ph cyclo-C5H9 C-463 CH3cyclo-C6H11 C-464 C2H5 cyclo-C6H11 C-465 n-C3H7 cyclo-C6H11 C-466 i-C3H7cyclo-C6H11 C-467 n-C4H9 cyclo-C6H11 C-468 s-C4H9 cyclo-C6H11 C-469i-C4H9 cyclo-C6H11 C-470 t-C4H9 cyclo-C6H11 C-471 n-C5H11 cyclo-C6H11C-472 n-C6H13 cyclo-C6H11 C-473 CH2CH═CH2 cyclo-C6H11 C-474CH2C(CH3)═CH2 cyclo-C6H11 C-475 CH2C(CH3)═CHCH3 cyclo-C6H11 C-476CH2CH═C(CH3)2 cyclo-C6H11 C-477 CH2CCl═CH2 cyclo-C6H11 C-478 CH2CH═CCl2cyclo-C6H11 C-479 CH2CH═CHCF3 cyclo-C6H11 C-480 CH2CH═CHPh cyclo-C6H11C-481 CH(CH3)CH═CH2 cyclo-C6H11 C-482 CH2CCH cyclo-C6H11 C-483 CH2CCCH3cyclo-C6H11 C-484 CH2CF3 cyclo-C6H11 C-485 CH2CH2OCH3 cyclo-C6H11 C-486CH2CH2OC2H5 cyclo-C6H11 C-487 CH2CH2CH2OCH3 cyclo-C6H11 C-488CH2CH2CH2OC2H5 cyclo-C6H11 C-489 CH2CH(OCH3)2 cyclo-C6H11 C-490 CH2CNcyclo-C6H11 C-491 CH2(cyclo-C3H5) cyclo-C6H11 C-492 CH2(cyclo-C5H9)cyclo-C6H11 C-493 CH2(cyclo-C6H11) cyclo-C6H11 C-494 CH2Ph cyclo-C6H11C-495 CH2(2-Cl-Ph) cyclo-C6H11 C-496 CH2(3-Cl-Ph) cyclo-C6H11 C-497CH2(4-Cl-Ph) cyclo-C6H11 C-498 CH2(2-CF3-Ph) cyclo-C6H11 C-499CH2(3-CF3-Ph) cyclo-C6H11 C-500 CH2(4-CF3-Ph) cyclo-C6H11 C-501CH2(2-F-Ph) cyclo-C6H11 C-502 CH2(3-F-Ph) cyclo-C6H11 C-503 CH2(4-F-Ph)cyclo-C6H11 C-504 CH2(2-OMe-Ph) cyclo-C6H11 C-505 CH2(3-OMe-Ph)cyclo-C6H11 C-506 CH2(4-OMe-Ph) cyclo-C6H11 C-507 CH(CH3)Ph cyclo-C6H11C-508 CH(CH3)(2-Cl-Ph) cyclo-C6H11 C-509 CH(CH3)(3-Cl-Ph) cyclo-C6H11C-510 CH(CH3)(4-Cl-Ph) cyclo-C6H11 C-511 CH(CH3)(2-CF3-Ph) cyclo-C6H11C-512 CH(CH3)(3-CF3-Ph) cyclo-C6H11 C-513 CH(CH3)(4-CF3-Ph) cyclo-C6H11C-514 CH2CH2Ph cyclo-C6H11 C-515 CH3 CH2Ph C-516 C2HS CH2Ph C-517 n-C3H7CH2Ph C-518 i-C3H7 CH2Ph C-519 n-C4H9 CH2Ph C-520 s-C4H9 CH2Ph C-521i-C4H9 CH2Ph C-522 t-C4H9 CH2Ph C-523 n-C5H11 CH2Ph C-524 n-C6H13 CH2PhC-525 CH2CH═CH2 CH2Ph C-526 CH2C(CH3)═CH2 CH2Ph C-527 CH2C(CH3)═CHCH3CH2Ph C-528 CH2CH═C(CH3)2 CH2Ph C-529 CH2CCl═CH2 CH2Ph C-530 CH2CH═CCl2CH2Ph C-531 CH2CH═CHCF3 CH2Ph C-532 CH2CH═CHPh CH2Ph C-533 CH(CH3)CH═CH2CH2Ph C-534 CH2CCH CH2Ph C-535 CH2CCCH3 CH2Ph C-536 CH2CF3 CH2Ph C-537CH2CH2OCH3 CH2Ph C-538 CH2CH2OC2H5 CH2Ph C-539 CH2CH2CH2OCH3 CH2Ph C-540CH2CH2CH2OC2H5 CH2Ph C-541 CH2CH(OCH3)2 CH2Ph C-542 CH2CN CH2Ph C-543CH2(cyclo-C3H5) CH2Ph C-544 CH2(cyclo-C5H9) CH2Ph C-545 CH2(cyclo-C6H11)CH2Ph C-546 CH2Ph CH2Ph C-547 CH2(2-Cl-Ph) CH2Ph C-548 CH2(3-Cl-Ph)CH2Ph C-549 CH2(4-Cl-Ph) CH2Ph C-550 CH2(2-CF3-Ph) CH2Ph C-551CH2(3-CF3-Ph) CH2Ph C-552 CH2(4-CF3-Ph) CH2Ph C-553 CH2(2-F-Ph) CH2PhC-554 CH2(3-F-Ph) CH2Ph C-555 CH2(4-F-Ph) CH2Ph C-556 CH2(2-OMe-Ph)CH2Ph C-557 CH2(3-OMe-Ph) CH2Ph C-558 CH2(4-OMe-Ph) CH2Ph C-559CH(CH3)Ph CH2Ph C-560 CH(CH3)(2-Cl-Ph) CH2Ph C-561 CH(CH3)(3-Cl-Ph)CH2Ph C-562 CH(CH3)(4-Cl-Ph) CH2Ph C-563 CH(CH3)(2-CF3-Ph) CH2Ph C-564CH(CH3)(3-CF3-Ph) CH2Ph C-565 CH(CH3)(4-CF3-Ph) CH2Ph C-566 CH2CH2PhCH2Ph C-567 n-C3H7 CH(CH3)Ph C-568 i-C3H7 CH(CH3)Ph C-569 CH2CH═CH2CH(CH3)Ph C-570 CH2O(CH3)═CH2 CH(CH3)Ph C-571 CH2C(CH3)═CHCH3 CH(CH3)PhC-572 CH2CH═C(CH3)2 CH(CH3)Ph C-573 CH2Ph CH(CH3)Ph C-574 CH2(3-CF3-Ph)CH(CH3)Ph C-575 n-C3H7 CH2(2-Ci-Ph) C-576 i-C3H7 CH2(2-Cl-Ph) C-577CH2CH═CH2 CH2(2-Cl-Ph) C-578 CH2C(CH3)═CH2 CH2(2-Cl-Ph) C-579CH2C(CH3)═CHCH3 CH2(2-Cl-Ph) C-580 CH2CH═C(CH3)2 CH2(2-Cl-Ph) C-581CH2Ph CH2(2-Cl-Ph) C-582 CH2(3-CF3-Ph) CH2(2-Cl-Ph) C-583 n-C3H7CH2(3-Cl-Ph) C-584 i-C3H7 CH2(3-Cl-Ph) C-585 CH2CH═CH2 CH2(3-Cl-Ph)C-586 CH2C(CH3)═CH2 CH2(3-Cl-Ph) C-587 CH2C(CH3)═CHCH3 CH2(3-Cl-Ph)C-588 CH2CH═C(CH3)2 CH2(3-Cl-Ph) C-589 CH2Ph CH2(3-Cl-Ph) C-590CH2(3-CF3-Ph) CH2(3-Cl-Ph) C-591 n-C3H7 CH2(4-Cl-Ph) C-592 i-C3H7CH2(4-Cl-Ph) C-593 CH2CH═CH2 CH2(4-Cl-Ph) C-594 CH2C(CH3)═CH2CH2(4-Cl-Ph) C-595 CH2C(CH3)═CHCH3 CH2(4-Cl-Ph) C-596 CH2CH═C(CH3)2CH2(4-Cl-Ph) C-597 CH2Ph CH2(4-Cl-Ph) C-598 CH2(3-CF3-Ph) CH2(4-Cl-Ph)C-599 n-C3H7 CH2(4-MeO-Ph) C-600 i-C3H7 CH2(4-MeO-Ph) C-601 CH2CH═CH2CH2(4-MeO-Ph) C-602 CH2C(CH3)═CH2 CH2(4-MeO-Ph) C-603 CH2C(CH3)═CHCH3CH2(4-MeO-Ph) C-604 CH2CH═C(CH3)2 CH2(4-MeO-Ph) C-605 CH2PhCH2(4-MeO-Ph) C-606 CH2(3-CF3-Ph) CH2(4-MeO-Ph) C-607 CH2CCHCH2CH2CH(OCH3)CH3 C-608 CH3 CH2CH2CH2SCH3 C-609 CH3 NHCH3 C-610 C2H5NHCH3 C-611 i-C3H7 NHCH3 C-612 CH2CH═CH2 NHCH3 C-613 CH2CCH NHCH3 C-614CH2Ph NHCH3 C-615 CH3 NHO2H5 C-616 C2H5 NHO2H5 C-617 i-C3H7 NHC2H5 C-618CH2CH═CH2 NHO2H5 C-619 CH2CCH NHC2H5 C-620 CH2Ph NHC2H5 C-621 CH3NH(i-C3H7) C-622 C2H5 NH(i-C3H7) C-623 i-C3H7 NH(i-C3H7) C-624 CH2CH═CH2NH(i-C3H7) C-625 CH2CCH NH(i-C3H7) C-626 CH2Ph NH(i-C3H7) C-627 CH3NH(t-C4H9) C-628 C2H5 NH(t-C4H9) C-629 i-C3H7 NH(t-C4H9) C-630 CH2CH═CH2NH(t-C4H9) C-631 CH2CCH NH(t-C4H9) C-632 CH2Ph NH(t-C4H9) C-633 CH3NH(cyclo-C6H11) C-634 C2H5 NH(cyclo-C6H11) C-635 i-C3H7 NH(cyclo-C6H11)C-636 CH2CH═CH2 NH(cyclo-C6H11) C-637 CH2CCH NH(cyclo-C6H11) C-638 CH2PhNH(cyclo-C6H11) C-639 CH3 NHCH2Ph C-640 C2H5 NHCH2Ph C-641 i-C3H7NHCH2Ph C-642 CH2CH═CH2 NHCH2Ph C-643 CH2CCH NHCH2Ph C-644 CH2Ph NHCH2PhC-645 CH3 NHPh C-646 C2H5 NHPh C-647 i-C3H7 NHPh C-648 t-C4H9 NHPh C-649CH2CCH NHPh C-650 CH2Ph NHPh C-651 CH2CCH CH2CH2CH(CH3)OCH3

TABLE 4 Compounds of formula (Id): (Id)

Compound Y R² R^(c) R^(d) R^(a) R^(b) D-1 S H H H H H D-2 S CH3 H H H HD-3 S C2H5 H H H H D-4 S n-C3H7 H H H H D-5 S i-C3H7 H H H H D-6 Sn-C4H9 H H H H D-7 S s-C4H9 H H H H D-8 S i-C4H9 H H H H D-9 S t-C4H9 HH H H D-10 S n-C5H11 H H H H D-11 S n-C6H13 H H H H D-12 S CH2CH═CH2 H HH H D-13 S CH2C(CH3)═CH2 H H H H D-14 S CH2C(CH3)═CHCH3 H H H H D-15 SCH2CH═C(CH3)2 H H H H D-16 S CH2CCl═CH2 H H H H D-17 S CH2CH═CCl2 H H HH D-18 S CH2CH═CHCF3 H H H H D-19 S CH(CH3)CH═CH2 H H H H D-20 S CH2CCHH H H H D-21 S CH2CCCH3 H H H H D-22 S CH2CF3 H H H H D-23 S CH2CH2OCH3H H H H D-24 S CH2CH2OC2H5 H H H H D-25 S CH2CH2CH2OCH3 H H H H D-26 SCH2CH2CH2OC2H5 H H H H D-27 S CH2CH(OCH3)2 H H H H D-28 S CH2CN H H H HD-29 S C(CH3)2CN H H H H D-30 S C(CH3)(i-C3H7)CN H H H H D-31 SCH2CO2CH3 H H H H D-32 S CH2CO2C2H5 H H H H D-33 S CH(CH3)CO2CH3 H H H HD-34 S cyclo-C3H7 H H H H D-35 S cyclo-C5H9 H H H H D-36 S cyclo-C6H11 HH H H D-37 S CH2(cyclo-C3H5) H H H H D-38 S CH2(cyclo-C5H9) H H H H D-39S CH2(cyclo-C6H11) H H H H D-40 S CH2Ph H H H H D-41 S CH2(2-Cl-Ph) H HH H D-42 S CH2(3-Cl-Ph) H H H H D-43 S CH2(4-Cl-Ph) H H H H D-44 SCH2(2-CF3-Ph) H H H H D-45 S CH2(3-CF3-Ph) H H H H D-46 S CH2(4-CF3-Ph)H H H H D-47 S CH2(2-F-Ph) H H H H D-48 S CH2(3-F-Ph) H H H H D-49 SCH2(4-F-Ph) H H H H D-50 S CH2(2-OMe-Ph) H H H H D-51 S CH2(3-OMe-Ph) HH H H D-52 S CH2(4-OMe-Ph) H H H H D-53 S CH(CH3)Ph H H H H D-54 SCH(CH3)(2-Cl-Ph) H H H H D-55 S CH(CH3)(3-Cl-Ph) H H H H D-56 SCH(CH3)(4-Cl-Ph) H H H H D-57 S CH(CH3)(2-CF3-Ph) H H H H D-58 SCH(CH3)(3-CF3-Ph) H H H H D-59 S CH(CH3)(4-CF3-Ph) H H H H D-60 S Ph H HH H D-61 S 2-Cl-Ph H H H H D-62 S 3-Cl-Ph H H H H D-63 S 4-Cl-Ph H H H HD-64 S 2-CF3-Ph H H H H D-65 S 3-CF3-Ph H H H H D-66 S 4-CF3-Ph H H H HD-67 S 2-CH3O-Ph H H H H D-68 S 3-CH3O-Ph H H H H D-69 S 4-CH3O-Ph H H HH D-70 S 4-CF3O-Ph H H H H D-71 S 4-CF3CH2O-Ph H H H H D-12 S 4-PhO-Ph HH H H D-73 S 4-(4-Cl-Ph)O-Ph H H H H D-74 S 4-(4-CF3-Ph)O-Ph H H H HD-75 S OCH3 H H H H D-76 S OC2H5 H H H H D-77 S O-n-C3H7 H H H H D-78 SO-i-C3H7 H H H H D-79 S O-n-C4H9 H H H H D-80 S O-i-C4H7 H H H H D-81 SO-sec-C4H9 H H H H D-82 S O-t-C4H9 H H H H D-83 S O-n-C5H11 H H H H D-84S OCH2CH═CH2 H H H H D-85 S OCH2C(CH3)═CH2 H H H H D-86 S OCH2CH═CHCH3 HH H H D-87 S OCH2CH═C(CH3)2 H H H H D-88 S OCH2CCH H H H H D-89 SOCH2CCCH3 H H H H D-90 S OCH2Ph H H H H D-91 S OCH(CH3)Ph H H H H D-92 SOCH2(2-Cl-Ph) H H H H D-93 S OCH2(3-Cl-Ph) H H H H D-94 S OCH2(4-Cl-Ph)H H H H D-95 S OCH2(2-OCH3-Ph) H H H H D-96 S OCH2(3-OCH3-Ph) H H H HD-97 S OCH2(4-OCH3-Ph) H H H H D-98 S OCH2(2-CF3-Ph) H H H H D-99 SOCH2(3-CF3-Ph) H H H H D-100 S OCH2(4-CF3-Ph) H H H H D-101 SOCH2(2-NO2-Ph) H H H H D-102 S OCH2(3-NO2-Ph) H H H H D-103 SOCH2(4-NO2-Ph) H H H H D-104 S CH3 O H H D-105 S C2H5 O H H D-106 Sn-C3H7 O H H D-107 S i-C3H7 O H H D-108 S n-C4H9 O H H D-109 S s-C4H9 OH H D-110 S i-C4H9 O H H D-111 S t-C4H9 O H H D-112 S n-C5H11 O H HD-113 S n-C6H13 O H H D-114 S CH2CH═CH2 O H H D-115 S CH2C(CH3)═CH2 O HH D-116 S CH2C(CH3)═CHCH3 O H H D-117 S CH2CH═C(CH3)2 O H H D-118 SCH2CCl═CH2 O H H D-119 S CH2CH═CCl2 O H H D-120 S CH2CH═CHCF3 O H HD-121 S CH2CH═CHPh O H H D-122 S CH(CH3)CH═CH2 O H H D-123 S CH2CCH O HH D-124 S CH2CCCH3 O H H D-125 S CH2CF3 O H H D-126 S CH2CH2OCH3 O H HD-127 S CH2CH2CO2H5 O H H D-128 S CH2CH2CH2OCH3 O H H D-129 SCH2CH2CH2OC2H5 O H H D-130 S CH2CH(OCH3)2 O H H D-131 S CH2CN O H HD-132 S C(CH3)2CN O H H D-133 S C(CH3)(i-C3H7)CN O H H D-134 S CH2CO2CH3O H H D-135 S CH2CO2C2H5 O H H D-136 S CH(CH3)CO2CH3 O H H D-137 Scyclo-C3H7 O H H D-138 S cyclo-C5H9 O H H D-139 S cyclo-C6H11 O H HD-140 S CH2(cyclo-C3H5) O H H D-141 S CH2(cyclo-C5H9) O H H D-142 SCH2(cyclo-C6H11) O H H D-143 S CH2Ph O H H D-144 S CH2(2-Cl-Ph) O H HD-145 S CH2(3-Cl-Ph) O H H D-146 S CH2(4-Cl-Ph) O H H D-147 SCH2(2-CF3-Ph) O H H D-148 S CH2(3-CF3-Ph) O H H D-149 S CH2(4-CF3-Ph) OH H D-150 S CH2(2-F-Ph) O H H D-151 S CH2(3-F-Ph) O H H D-152 SCH2(4-F-Ph) O H H D-153 S CH2(2-OMe-Ph) O H H D-154 S CH2(3-OMe-Ph) O HH D-155 S CH2(4-OMe-Ph) O H H D-156 S CH(CH3)Ph O H H D-157 SCH(CH3)(2-Cl-Ph) O H H D-158 S CH(CH3)(3-Cl-Ph) O H H D-159 SCH(CH3)(4-Cl-Ph) O H H D-160 S CH(CH3)(2-CF3-Ph) O H H D-161 SCH(CH3)(3-CF3-Ph) O H H D-162 S CH(CH3)(4-CF3-Ph) O H H D-163 S Ph O H HD-164 S 2-Cl-Ph O H H D-165 S 3-Cl-Ph O H H D-166 S 4-Cl-Ph O H H D-167S 2-CF3-Ph O H H D-168 S 3-CF3-Ph O H H D-169 S 4-CF3-Ph O H H D-170 S2-CH3O-Ph O H H D-171 S 3-CH3O-Ph O H H D-172 S 4-CH3O-Ph O H H D-173 S4-CF3O-Ph O H H D-174 S 4-CF3CH2O-Ph O H H D-175 S 4-PhO-Ph O H H D-176S 4-(4-Cl-Ph)O-Ph O H H D-177 S 4-(4-CF3-Ph)O-Ph O H H D-178 S OCH3 O HH D-179 S OC2H5 O H H D-180 S O-n-C3H7 O H H D-181 S O-i-C3H7 O H HD-182 S O-n-C4H9 O H H D-183 S O-i-C4H7 O H H D-184 S O-sec-C4H9 O H HD-185 S O-t-C4H9 O H H D-186 S O-n-C5H11 O H H D-187 S OCH2CH═CH2 O H HD-188 S OCH2C(CH3)CH2 O H H D-189 S OCH2CH═CHCH3 O H H D-190 SOCH2CH═C(CH3)2 O H H D-191 S OCH2CCH O H H D-192 S OCH2CCCH3 O H H D-193S OCH2Ph O H H D-194 S OCH(CH3)Ph O H H D-195 S OCH2(2-Cl-Ph) O H HD-196 S OCH2(3-Cl-Ph) O H H D-197 S OCH2(4-Cl-Ph) O H H D-198 SOCH2(2-OCH3-Ph) O H H D-199 S OCH2(3-OCH3-Ph) O H H D-200 SOCH2(4-OCH3-Ph) O H H D-201 S OCH2(2-CF3-Ph) O H H D-202 SOCH2(3-CF3-Ph) O H H D-203 S OCH2(4-CF3-Ph) O H H D-204 S OCH2(2-NO2-Ph)O H H D-205 S OCH2(3-NO2-Ph) O H H D-206 S OCH2(4-NO2-Ph) O H H D-207 SCH3 O CH3 H D-208 S C2H5 O CH3 H D-209 S n-C3H7 O CH3 H D-210 S i-C3H7 OCH3 H D-211 S n-C4H9 O CH3 H D-212 S s-C4H9 O CH3 H D-213 S i-C4H9 O CH3H D-214 S t-C4H9 O CH3 H D-215 S n-C5H11 O CH3 H D-216 S n-C6H13 O CH3 HD-217 S CH2CH═CH2 O CH3 H D-218 S CH2C(CH3)═CH2 O CH3 H D-219 SCH2C(CH3)═CHCH3 O CH3 H D-220 S CH2CH═C(CH3)2 O CH3 H D-221 S CH2CCl═CH2O CH3 H D-222 S CH2CH═CCl2 O CH3 H D-223 S CH2CH═CHCF3 O CH3 H D-224 SCH2CH═CHPh O CH3 H D-225 S CH(CH3)CH═CH2 O CH3 H D-226 S CH2CCH O CH3 HD-227 S CH2CCCH3 O CH3 H D-228 S CH2CF3 O CH3 H D-229 S CH2CH2OCH3 O CH3H D-230 S CH2CH2CO2H5 O CH3 H D-231 S CH2CH2CH2OCH3 O CH3 H D-232 SCH2CH2CH2CO2H5 O CH3 H D-233 S CH2CH(OCH3)2 O CH3 H D-234 S CH2CN O CH3H D-235 S C(CH3)2CN O CH3 H D-236 S C(CH3)(i-C3H7)CN O CH3 H D-237 SCH2CO2CH3 O CH3 H D-238 S CH2CO2C2H5 O CH3 H D-239 S CH(CH3)CO2CH3 O CH3H D-240 S cyclo-C3H7 O CH3 H D-241 S cyclo-C5H9 O CH3 H D-242 Scyclo-C6H11 O CH3 H D-243 S CH2(cyclo-C3H5) O CH3 H D-244 SCH2(cyclo-C5H9) O CH3 H D-245 S CH2(cyclo-C6H11) O CH3 H D-246 S CH2Ph OCH3 H D-247 S CH2(2-Cl-Ph) O CH3 H D-248 S CH2(3-Cl-Ph) O CH3 H D-249 SCH2(4-Cl-Ph) O CH3 H D-250 S CH2(2-CF3-Ph) O CH3 H D-251 S CH2(3-CF3-Ph)O CH3 H D-252 S CH2(4-CF3-Ph) O CH3 H D-253 S CH2(2-F-Ph) O CH3 H D-254S CH2(3-F-Ph) O CH3 H D-255 S CH2(4-F-Ph) O CH3 H D-256 S CH2(2-OMe-Ph)O CH3 H D-257 S CH2(3-OMe-Ph) O CH3 H D-258 S CH2(4-OMe-Ph) O CH3 HD-259 S CH(CH3)Ph O CH3 H D-260 S CH(CH3)(2-Cl-Ph) O CH3 H D-261 SCH(CH3)(3-Cl-Ph) O CH3 H D-262 S CH(CH3)(4-Cl-Ph) O CH3 H D-263 SCH(CH3)(2-CF3-Ph) O CH3 H D-264 S CH(CH3)(3-CF3-Ph) O CH3 H D-265 SCH(CH3)(4-CF3-Ph) O CH3 H D-266 S Ph O CH3 H D-267 S 2-Cl-Ph O CH3 HD-268 S 3-Cl-Ph O CH3 H D-269 S 4-Cl-Ph O CH3 H D-270 S 2-CF3-Ph O CH3 HD-271 S 3-CF3-Ph O CH3 H D-272 S 4-CF3-Ph O CH3 H D-273 S 2-CH3O-Ph OCH3 H D-274 S 3-CH3O-Ph O CH3 H D-275 S 4-CH3O-Ph O CH3 H D-276 S4-CF3O-Ph O CH3 H D-271 S 4-CF3CH2O-Ph O CH3 H D-278 S 4-PhO-Ph O CH3 HD-279 S 4-(4-Cl-Ph)O-Ph O CH3 H D-280 S 4-(4-CF3-Ph)O-Ph O CH3 H D-281 SOCH3 O CH3 H D-282 S OC2H5 O CH3 H D-283 S O-n-C3H7 O CH3 H D-284 SO-i-C3H7 O CH3 H D-285 S O-n-C4H9 O CH3 H D-286 S O-i-C4H7 O CH3 H D-287S O-sec-C4H9 O CH3 H D-288 S O-t-C4H9 O CH3 H D-289 S O-n-C5H11 O CH3 HD-290 S OCH2CH═CH2 O CH3 H D-291 S OCH2C(CH3)═CH2 O CH3 H D-292 SOCH2CH═CHCH3 O CH3 H D-293 S OCH2CH═C(CH3)2 O CH3 H D-294 S OCH2CCH OCH3 H D-295 S OCH2CCCH3 O CH3 H D-296 S OCH2Ph O CH3 H D-297 SOCH(CH3)Ph O CH3 H D-298 S OCH2(2-Cl-Ph) O CH3 H D-299 S OCH2(3-Cl-Ph) OCH3 H D-300 S OCH2(4-Cl-Ph) O CH3 H D-301 S OCH2(2-OCH3-Ph) O CH3 HD-302 S OCH2(3-OCH3-Ph) O CH3 H D-303 S OCH2(4-OCH3-Ph) O CH3 H D-304 SOCH2(2-CF3-Ph) O CH3 H D-305 S OCH2(3-CF3-Ph) O CH3 H D-306 SOCH2(4-CF3-Ph) O CH3 H D-307 S OCH2(2-NO2-Ph) O CH3 H D-308 SOCH2(3-NO2-Ph) O CH3 H D-309 S OCH2(4-NO2-Ph) O CH3 H D-310 S CH3 O CH3CH3 D-311 S C2H5 O CH3 CH3 D-312 S n-C3H7 O CH3 CH3 D-313 S i-C3H7 O CH3CH3 D-314 S n-C4H9 O CH3 CH3 D-315 S s-C4H9 O CH3 CH3 D-316 S i-C4H9 OCH3 CH3 D-317 S t-C4H9 O CH3 CH3 D-318 S n-C5H1I O CH3 CH3 D-319 Sn-C6H13 O CH3 CH3 D-320 S CH2CH═CH2 O CH3 CH3 D-321 S CH2C(CH3)═CH2 OCH3 CH3 D-322 S CH2C(CH3)═CHCH3 O CH3 CH3 D-323 S CH2CH═C(CH3)2 O CH3CH3 D-324 S CH2CCl═CH2 O CH3 CH3 D-325 S CH2CH═CCl2 O CH3 CH3 D-326 SCH2CH═CHCF3 O CH3 CH3 D-327 S CH2CH═CHPh O CH3 CH3 D-328 S CH(CH3)CH═CH2O CH3 CH3 D-329 S CH2CCH O CH3 CH3 D-330 S CH2CCCH3 O CH3 CH3 D-331 SCH2CF3 O CH3 CH3 D-332 S CH2CH2OCH3 O CH3 CH3 D-333 S CH2CH2OC2H5 O CH3CH3 D-334 S CH2CH2CH2OCH3 O CH3 CH3 D-335 S CH2CH2CH2OC2H5 O CH3 CH3D-336 S CH2CH(OCH3)2 O CH3 CH3 D-337 S CH2CN O CH3 CH3 D-338 S C(CH3)2CNO CH3 CH3 D-339 S C(CH3)(i-C3H7)CN O CH3 CH3 D-340 S CH2CO2CH3 O CH3 CH3D-341 S CH2CO2C2H5 O CH3 CH3 D-342 S CH(CH3)CO2CH3 O CH3 CH3 D-343 Scyclo-C3H7 O CH3 CH3 D-344 S cyclo-C5H9 O CH3 CH3 D-345 S cyclo-C6H11 OCH3 CH3 D-346 S CH2(cyclo-C3H5) O CH3 CH3 D-347 S CH2(cyclo-C5H9) O CH3CH3 D-348 S CH2(cyclo-C6H11) O CH3 CH3 D-349 S CH2Ph O CH3 CH3 D-350 SCH2(2-Cl-Ph) O CH3 CH3 D-351 S CH2(3-Cl-Ph) O CH3 CH3 D-352 SCH2(4-Cl-Ph) O CH3 CH3 D-353 S CH2(2-CF3-Ph) O CH3 CH3 D-354 SCH2(3-CF3-Ph) O CH3 CH3 D-355 S CH2(4-CF3-Ph) O CH3 CH3 D-356 SCH2(2-F-Ph) O CH3 CH3 D-357 S CH2(3-F-Ph) O CH3 CH3 D-358 S CH2(4-F-Ph)O CH3 CH3 D-359 S CH2(2-OMe-Ph) O CH3 CH3 D-360 S CH2(3-OMe-Ph) O CH3CH3 D-361 S CH2(4-0Me-Ph) O CH3 CH3 D-362 S CH(CH3)Ph O CH3 CH3 D-363 SCH(CH3)(2-Cl-Ph) O CH3 CH3 D-364 S CH(CH3)(3-Cl-Ph) O CH3 CH3 D-365 SCH(CH3)(4-Cl-Ph) O CH3 CH3 D-366 S CH(CH3)(2-CF3-Ph) O CH3 CH3 D-367 SCH(CH3)(3-CF3-Ph) O CH3 CH3 D-368 S CH(CH3)(4-CF3-Ph) O CH3 CH3 D-369 SPh O CH3 CH3 D-370 S 2-Cl-Ph O CH3 CH3 D-371 S 3-Cl-Ph O CH3 CH3 D-372 S4-Cl-Ph O CH3 CH3 D-373 S 2-CF3-Ph O CH3 CH3 D-374 S 3-CF3-Ph O CH3 CH3D-375 S 4-CF3-Ph O CH3 CH3 D-376 S 2-CH3O-Ph O CH3 CH3 D-377 S 3-CH3O-PhO CH3 CH3 D-378 S 4-CH3O-Ph O CH3 CH3 D-379 S 4-CF3O-Ph O CH3 CH3 D-380S 4-CF3CH2O-Ph O CH3 CH3 D-381 S 4-PhO-Ph O CH3 CH3 D-382 S4-(4-Cl-Ph)O-Ph O CH3 CH3 D-383 S 4-(4-CF3-Ph)O-Ph O CH3 CH3 D-384 SOCH3 O CH3 CH3 D-385 S OC2H5 O CH3 CH3 D-386 S O-n-C3H7 O CH3 CH3 D-387S D-i-C3H7 O CH3 CH3 D-388 S O-n-C4H9 O CH3 CH3 D-389 S O-i-C4H7 O CH3CH3 D-390 S O-sec-C4H9 O CH3 CH3 D-391 S O-t-C4H9 O CH3 CH3 D-392 SO-n-C5H11 O CH3 CH3 D-393 S OCH2CH═CH2 O CH3 CH3 D-394 S OCH2C(CH3)═CH2O CH3 CH3 D-395 S OCH2CH═CHCH3 O CH3 CH3 D-396 S OCH2CH═C(CH3)2 O CH3CH3 D-397 S OCH2CCH O CH3 CH3 D-398 S OCH2CCCH3 O CH3 CH3 D-399 S OCH2PhO CH3 CH3 D-400 S OCH(CH3)Ph O CH3 CH3 D-401 S OCH2(2-Cl-Ph) O CH3 CH3D-402 S OCH2(3-Cl-Ph) O CH3 CH3 D-403 S OCH2(4-Cl-Ph) O CH3 CH3 D-404 SOCH2(2-OCH3-Ph) O CH3 CH3 D-405 S OCH2(3-OCH3-Ph) O CH3 CH3 D-406 SOCH2(4-OCH3-Ph) O CH3 CH3 D-407 S OCH2(2-CF3-Ph) O CH3 CH3 D-408 SOCH2(3-CF3-Ph) O CH3 CH3 D-409 S OCH2(4-CF3-Ph) O CH3 CH3 D-410 SOCH2(2-NO2-Ph) O CH3 CH3 D-411 S OCH2(3-NO2-Ph) O CH3 CH3 D-412 SOCH2(4-NO2-Ph) O CH3 CH3 D-413 S CH3 O C2H5 H D-414 S C2H5 O C2H5 HD-415 S n-C3H7 O C2H5 H D-416 S i-C3H7 O C2H5 H D-417 S n-C4H9 O C2H5 HD-418 S s-C4H9 O C2H5 H D-419 S i-C4H9 O C2H5 H D-420 S t-C4H9 O C2H5 HD-421 S n-C5H11 O C2H5 H D-422 S n-C6H13 O C2H5 H D-423 S CH2CH═CH2 OC2H5 H D-424 S CH2C(CH3)═CH2 O C2H5 H D-425 S CH2C(CH3)═CHCH3 O C2H5 HD-426 S CH2CH═C(CH3)2 O C2H5 H D-427 S CH2CCl═CH2 O C2H5 H D-428 SCH2CH═CCl2 O C2H5 H D-429 S CH2CH═CHCF3 O C2H5 H D-430 S CH2CH═CHPh OC2H5 H D-431 S CH(CH3)CH═CH2 O C2H5 H D-432 S CH2CCH O C2H5 H D-433 SCH2CCCH3 O C2H5 H D-434 S CH2CF3 O C2H5 H D-435 S CH2CH2OCH3 O C2H5 HD-436 S CH2CH2CO2H5 O C2H5 H D-437 S CH2CH2CH2OCH3 O C2H5 H D-438 SCH2CH2CH2OC2H5 O C2H5 H D-439 S CH2CH(OCH3)2 O C2H5 H D-440 S CH2CN OC2H5 H D-441 S C(CH3)2CN O C2H5 H D-442 S C(CH3)(i-C3H7)CN O C2H5 HD-443 S CH2CO2CH3 O C2H5 H D-444 S CH2CO2C2H5 O C2H5 H D-445 SCH(CH3)CO2CH3 O C2H5 H D-446 S cyclo-C3H7 O C2H5 H D-447 S cyclo-C5H9 OC2H5 H D-448 S cyclo-C6H11 O C2H5 H D-449 S CH2(cyclo-C3H5) O C2H5 HD-450 S CH2(cyclo-C5H9) O C2H5 H D-451 S CH2(cyclo-C6H11) O C2H5 H D-452S CH2Ph O C2H5 H D-453 S CH2(2-Cl-Ph) O C2H5 H D-454 S CH2(3-Cl-Ph) OC2H5 H D-455 S CH2(4-Cl-Ph) O C2H5 H D-456 S CH2(2-CF3-Ph) O C2H5 HD-457 S CH2(3-CF3-Ph) O C2H5 H D-458 S CH2(4-CF3-Ph) O C2H5 H D-459 SCH2(2-F-Ph) O C2H5 H D-460 S CH2(3-F-Ph) O C2H5 H D-461 S CH2(4-F-Ph) OC2H5 H D-462 S CH2(2-OMe-Ph) O C2H5 H D-463 S CH2(3-OMe-Ph) O C2H5 HD-464 S CH2(4-OMe-Ph) O C2H5 H D-465 S CH(CH3)Ph O C2H5 H D-466 SCH(CH3)(2-Cl-Ph) O C2H5 H D-467 S CH(CH3)(3-Cl-Ph) O C2H5 H D-468 SCH(CH3)(4-Cl-Ph) O C2H5 H D-469 S CH(CH3)(2-CF3-Ph) O C2H5 H D-470 SCH(CH3)(3-CF3-Ph) O C2H5 H D-471 S CH(CH3)(4-CF3-Ph) O C2H5 H D-472 S PhO C2H5 H D-473 S 2-Cl-Ph O C2H5 H D-474 S 3-Cl-Ph O C2H5 H D-475 S4-Cl-Ph O C2H5 H D-476 S 2-CF3-Ph O C2H5 H D-477 S 3-CF3-Ph O C2H5 HD-478 S 4-CF3-Ph O C2H5 H D-479 S 2-CH3O-Ph O C2H5 H D-480 S 3-CH3O-Ph OC2H5 H D-481 S 4-CH3O-Ph O C2H5 H D-482 S 4-CF3O-Ph O C2H5 H D-483 S4-CF3CH2O-Ph O C2H5 H D-484 S 4-PhO-Ph O C2H5 H D-485 S 4-(4-Cl-Ph)O-PhO C2H5 H D-486 S 4-(4-CF3-Ph)O-Ph O C2H5 H D-487 S OCH3 O C2H5 H D-488 SOC2H5 O C2H5 H D-489 S O-n-C3H7 O C2H5 H D-490 S O-i-C3H7 O C2H5 H D-491S O-n-C4H9 O C2H5 H D-492 S O-i-C4H7 O C2H5 H D-493 S O-sec-C4H9 O C2H5H D-494 S O-t-C4H9 O C2H5 H D-495 S O-n-C5H11 O C2H5 H D-496 SOCH2CH═CH2 O C2H5 H D-497 S OCH2C(CH3)═CH2 O C2H5 H D-498 S OCH2CH═CHCH3O C2H5 H D-499 S OCH2CH═C(CH3)2 O C2H5 H D-500 S OCH2CCH O C2H5 H D-501S OCH2CCCH3 O C2H5 H D-502 S OCH2Ph O C2H5 H D-503 S OCH(CH3)Ph O C2H5 HD-504 S OCH2(2-Cl-Ph) O C2H5 H D-505 S OCH2(3-Cl-Ph) O C2H5 H D-506 SOCH2(4-Cl-Ph) O C2H5 H D-507 S OCH2(2-OCH3-Ph) O C2H5 H D-508 SOCH2(3-OCH3-Ph) O C2H5 H D-509 S OCH2(4-OCH3-Ph) O C2H5 H D-510 SOCH2(2-CF3-Ph) O C2H5 H D-511 S OCH2(3-CF3-Ph) O C2H5 H D-512 SOCH2(4-CF3-Ph) O C2H5 H D-513 S OCH2(2-NO2-Ph) O C2H5 H D-514 SOCH2(3-NO2-Ph) O C2H5 H D-515 S OCH2(4-NO2-Ph) O C2H5 H D-516 S CH3 Oi-C3H7 H D-517 S C2H5 O i-C3H7 H D-518 S n-C3H7 O i-C3H7 H D-519 Si-C3H7 O i-C3H7 H D-520 S n-C4H9 O i-C3H7 H D-521 S s-C4H9 O i-C3H7 HD-522 S i-C4H9 O i-C3H7 H D-523 S t-C4H9 O i-C3H7 H D-524 S n-C5H11 Oi-C3H7. H D-525 S n-C6H13 O i-C3H7 H D-526 S CH2CH═CH2 O i-C3H7 H D-527S CH2C(CH3)═CH2 O i-C3H7 H D-528 S CH2C(CH3)═CHCH3 O i-C3H7 H D-529 SCH2CH═C(CH3)2 O i-C3H7 H D-53O S CH2CCl═CH2 O i-C3H7 H D-531 SCH2CH═CCl2 O i-C3H7 H D-532 S CH2CH═CHCF3 O i-C3H7 H D-533 S CH2CH═CHPhO i-C3H7 H D-534 S CH(CH3)CH═CH2 O i-C3H7 H D-535 S CH2CCH O i-C3H7 HD-536 S CH2CCCH3 O i-C3H7 H D-537 S CH2CF3 O i-C3H7 H D-538 S CH2CH2OCH3O i-C3H7 H D-539 S CH2CH2OC2H5 O i-C3H7 H D-540 S CH2CH2CH2OCH3 O i-C3H7H D-541 S CH2CH2CH2OC2H5 O i-C3H7 H D-542 S CH2CH(OCH3)2 O i-C3H7 HD-543 S CH2CN O i-C3H7 H D-544 S C(CH3)2CN O i-C3H7 H D-545 SC(CH3)(i-C3H7)CN O i-C3H7 H D-546 S CH2CO2CH3 O i-C3H7 H D-547 SCH2CO2C2H5 O i-C3H7 H D-548 S CH(CH3)CO2CH3 O i-C3H7 H D-549 Scyclo-C3H7 O i-C3H7 H D-550 S cyclo-C5H9 O i-C3H7 H D-551 S cyclo-C6H11O i-C3H7 H D-552 S CH2(cyclo-C3H5) O i-C3H7 H D-553 S CH2(cyclo-C5H9) Oi-C3H7 H D-554 S CH2(cyclo-C6H11) O i-C3H7 H D-555 S CH2Ph O i-C3H7 HD-556 S CH2(2-Cl-Ph) O i-C3H7 H D-557 S CH2(3-Cl-Ph) O i-C3H7 H D-558 SCH2(4-Cl-Ph) O i-C3H7 H D-559 S CH2(2-CF3-Ph) O i-C3H7 H D-560 SCH2(3-CF3-Ph) O i-C3H7 H D-561 S CH2(4-CF3-Ph) O i-C3H7 H D-562 SCH2(2-F-Ph) O i-C3H7 H D-563 S CH2(3-F-Ph) O i-C3H7 H D-564 SCH2(4-F-Ph) O i-C3H7 H D-565 S CH2(2-OMe-Ph) O i-C3H7 H D-566 SCH2(3-OMe-Ph) O i-C3H7 H D-567 S CH2(4-OMe-Ph) O i-C3H7 H D-568 SCH(CH3)Ph O i-C3H7 H D-569 S CH(CH3)(2-Cl-Ph) O i-C3H7 H D-570 SCH(CH3)(3-Cl-Ph) O i-C3H7 H D-571 S CH(CH3)(4-Cl-Ph) O i-C3H7 H D-572 SCH(CH3)(2-CF3-Ph) O i-C3H7 H D-573 S CH(CH3)(3-CF3-Ph) O i-C3H7 H D-574S CH(CH3)(4-CF3-Ph) O i-C3H7 H D-575 S Ph O i-C3H7 H D-576 S 2-Cl-Ph Oi-C3H7 H D-577 S 3-Cl-Ph O i-C3H7 H D-578 S 4-Cl-Ph O i-C3H7 H D-579 S2-CF3-Ph O i-C3H7 H D-580 S 3-CF3-Ph O i-C3H7 H D-581 S 4-CF3-Ph Oi-C3H7 H D-582 S 2-CH3O-Ph O i-C3H7 H D-583 S 3-CH3O-Ph O i-C3H7 H D-584S 4-CH3O-Ph O i-C3H7 H D-585 S 4-CF3O-Ph O i-C3H7 H D-586 S 4-CF3CH2O-PhO i-C3H7 H D-587 S 4-PhO-Ph O i-C3H7 H D-588 S 4-(4-Cl-Ph)O-Ph O i-C3H7H D-589 S 4-(4-CF3-Ph)O-Ph O i-C3H7 H D-590 S OCH3 O i-C3H7 H D-591 SOC2H5 O i-C3H7 H D-592 S O-n-C3H7 O i-C3H7 H D-593 S O-i-C3H7 O i-C3H7 HD-594 S O-n-C4H9 O i-C3H7 H D-595 S O-i-C4H7 O i-C3H7 H D-596 SO-sec-C4H9 O i-C3H7 H D-597 S O-t-C4H9 O i-C3H7 H D-598 S O-n-C5H11 Oi-C3H7 H D-599 S OCH2CH═CH2 O i-C3H7 H D-600 S OCH2C(CH3)═CH2 O i-C3H7 HD-601 S OCH2CH═CHCH3 O i-C3H7 H D-602 S OCH2CH═C(CH3)2 O i-C3H7 H D-603S OCH2CCH O i-C3H7 H D-604 S OCH2CCCH3 O i-C3H7 H D-605 S OCH2Ph Oi-C3H7 H D-606 S OCH(CH3)Ph O i-C3H7 H D-607 S OCH2(2-Cl-Ph) O i-C3H7 HD-608 S OCH2(3-Cl-Ph) O i-C3H7 H D-609 S OCH2(4-Cl-Ph) O i-C3H7 H D-610S OCH2(2-OCH3-Ph) O i-C3H7 H D-611 S OCH2(3-OCH3-Ph) O i-C3H7 H D-612 SOCH2(4-OCH3-Ph) O i-C3H7 H D-613 S OCH2(2-CF3-Ph) O i-C3H7 H D-614 SOCH2(3-CF3-Ph) O i-C3H7 H D-615 S OCH2(4-CF3-Ph) O i-C3H7 H D-616 SOCH2(2-NO2-Ph) O i-C3H7 H D-617 S OCH2(3-NO2-Ph) O i-C3H7 H D-618 SOCH2(4-NO2-Ph) O i-C3H7 H D-619 S CH3 O Ph H D-620 S C2H5 O Ph H D-621 Sn-C3H7 O Ph H D-622 S i-C3H7 O Ph H D-623 S n-C4H9 O Ph H D-624 S s-C4H9O Ph H D-625 S i-C4H9 O Ph H D-626 S t-C4H9 O Ph H D-627 S n-C5H11 O PhH D-628 S n-C6H13 O Ph H D-629 S CH2CH═CH2 O Ph H D-630 S CH2C(CH3)═CH2O Ph H D-631 S CH2C(CH3)═CHCH3 O Ph H D-632 S CH2CH═C(CH3)2 O Ph H D-633S CH2CCl═CH2 O Ph H D-634 S CH2CH═CCl2 O Ph H D-635 S CH2CH═CHCF3 O Ph HD-636 S CH2CH═CHPh O Ph H D-637 S CH(CH3)CH═CH2 O Ph H D-638 S CH2CCH OPh H D-639 S CH2CCCH3 O Ph H D-640 S CH2CF3 O Ph H D-641 S CH2CH2OCH3 OPh H D-642 S CH2CH2OC2H5 O Ph H D-643 S CH2CH2CH2OCH3 O Ph H D-644 SCH2CH2CH2OC2H5 O Ph H D-645 S CH2CH(OCH3)2 O Ph H D-646 S CH2CN O Ph HD-647 S C(CH3)2CN O Ph H D-648 S C(CH3)(i-C3H7)CN O Ph H D-649 SCH2CO2CH3 O Ph H D-650 S CH2CO2C2H5 O Ph H D-651 S CH(CH3)CO2CH3 O Ph HD-652 S cyclo-C3H7 O Ph H D-653 S cyclo-C5H9 O Ph H D-654 S cyclo-C6H11O Ph H D-655 S CH2(cyclo-C3H5) O Ph H D-656 S CH2(cyclo-C5H9) O Ph HD-657 S CH2(cyclo-C6H11) O Ph H D-658 S CH2Ph O Ph H D-659 SCH2(2-Cl-Ph) O Ph H D-660 S CH2(3-Cl-Ph) O Ph H D-661 S CH2(4-Cl-Ph) OPh H D-662 S CH2(2-CF3-Ph) O Ph H D-663 S CH2(3-CF3-Ph) O Ph H D-664 SCH2(4-CF3-Ph) O Ph H D-665 S CH2(2-F-Ph) O Ph H D-666 S CH2(3-F-Ph) O PhH D-667 S CH2(4-F-Ph) O Ph H D-668 S CH2(2-OMe-Ph) O Ph H D-669 SCH2(3-OMe-Ph) O Ph H D-670 S CH2(4-OMe-Ph) O Ph H D-671 S CH(CH3)Ph O PhH D-672 S CH(CH3)(2-Cl-Ph) O Ph H D-673 S CH(CH3)(3-Cl-Ph) O Ph H D-674S CH(CH3)(4-Cl-Ph) O Ph H D-675 S CH(CH3)(2-CF3-Ph) O Ph H D-676 SCH(CH3)(3-CF3-Ph) O Ph H D-677 S CH(CH3)(4-CF3-Ph) O Ph H D-678 S Ph OPh H D-619 S 2-Cl-Ph O Ph H D-680 S 3-Cl-Ph O Ph H D-681 S 4-Cl-Ph O PhH D-682 S 2-CF3-Ph O Ph H D-683 S 3-CF3-Ph O Ph H D-684 S 4-CF3-Ph O PhH D-685 S 2-CH3O-Ph O Ph H D-686 S 3-CH3O-Ph O Ph H D-687 S 4-CH3O-Ph OPh H D-688 S 4-CF3O-Ph O Ph H D-689 S 4-CF3CH2O-Ph O Ph H D-690 S4-PhO-Ph O Ph H D-691 S 4-(4-Cl-Ph)O-Ph O Ph H D-692 S 4-(4-CF3-Ph)O-PhO Ph H D-693 S OCH3 O Ph H D-694 S OC2H5 O Ph H D-695 S O-n-C3H7 O Ph HD-696 S O-i-C3H7 O Ph H D-697 S O-n-C4H9 O Ph H D-698 S O-i-C4H7 O Ph HD-699 S O-sec-C4H9 O Ph H D-700 S O-t-C4H9 O Ph H D-701 S O-n-C5H11 O PhH D-702 S OCH2CH═CH2 O Ph H D-703 S OCH2C(CH3)═CH2 O Ph H D-704 SOCH2CH═CHCH3 O Ph H D-705 S OCHCH═C(CH3)2 O Ph H D-706 S OCH2CCH O Ph HD-707 S OCH2CCCH3 O Ph H D-708 S OCH2Ph O Ph H D-709 S OCH(CH3)Ph O Ph HD-710 S OCH2(2-Cl-Ph) O Ph H D-711 S OCH2(3-Cl-Ph) O Ph H D-712 SOCH2(4-Cl-Ph) O Ph H D-713 S OCH2(2-OCH3-Ph) O Ph H D-714 SOCH2(3-OCH3-Ph) O Ph H D-715 S OCH2(4-OCH3-Ph) O Ph H D-716 SOCH2(2-CF3-Ph) O Ph H D-717 S OCH2(3-CF3-Ph) O Ph H D-718 SOCH2(4-CF3-Ph) O Ph H D-719 S OCH2(2-NO2-Ph) O Ph H D-720 SOCH2(3-NO2-Ph) O Ph H D-721 S OCH2(4-NO2-Ph) O Ph H D-722 S CH3 H HOC2H5 H D-723 S C2H5 H H OC2H5 H D-724 S n-C3H7 H H OC2H5 H D-725 Si-C3H7 H H OC2H5 H D-726 S n-C4H9 H H OC2H5 H D-727 S s-C4H9 H H OC2H5 HD-728 S i-C4H9 H H OC2H5 H D-729 S t-C4H9 H H OC2H5 H D-730 S n-C5H11 HH OC2H5 H D-731 S n-C6H13 H H OC2H5 H D-732 S CH2CH═CH2 H H OC2H5 HD-733 S CH2C(CH3)═CH2 H H OC2H5 H D-734 S CH2C(CH3)═CHCH3 H H OC2H5 HD-735 S CH2CH═C(CH3)2 H H OC2H5 H D-736 S CH2CCl═CH2 H H OC2H5 H D-737 SCH2CH═CCl2 H H OC2H5 H D-738 S CH2CH═CHCF3 H H OC2H5 H D-739 SCH2CH═CHPh H H OC2H5 H D-740 S CH(CH3)CH═CH2 H H OC2H5 H D-741 S CH2CCHH H OC2H5 H D-742 S CH2CCCH3 H H OC2H5 H D-743 S CH2CF3 H H OC2H5 HD-744 S CH2CH2OCH3 H H OC2H5 H D-745 S CH2CH2OC2H5 H H OC2H5 H D-746 SCH2CH2CH2OCH3 H H OC2H5 H D-747 S CH2CH2CH2CO2H5 H H OC2H5 H D-748 SCH2CH(OCH3)2 H H OC2H5 H D-749 S CH2CN H H OC2H5 H D-750 S C(CH3)2CN H HOC2H5 H D-751 S C(CH3)(i-C3H7)CN H H OC2H5 H D-752 S CH2CO2CH3 H H OC2H5H D-753 S CH2CO2C2H5 H H OC2H5 H D-754 S CH(CH3)CO2CH3 H H OC2H5 H D-755S cyclo-C3H7 H H OC2H5 H D-756 S cyclo-C5H9 H H OC2H5 H D-757 Scyclo-C6H11 H H OC2H5 H D-758 S CH2(cyclo-C3H5) H H OC2H5 H D-759 SCH2(cyclo-C5H9) H H OC2H5 H D-760 S CH2(cyclo-C6H11) H H OC2H5 H D-761 SCH2Ph H H OC2H5 H D-762 S CH2(2-Cl-Ph) H H OC2H5 H D-763 S CH2(3-Cl-Ph)H H OC2H5 H D-764 S CH2(4-Cl-Ph) H H OC2H5 H D-765 S CH2(2-CF3-Ph) H HOC2H5 H D-766 S CH2(3-CF3-Ph) H H OC2H5 H D-767 S CH2(4-CF3-Ph) H HOC2H5 H D-768 S CH2(2-F-Ph) H H OC2H5 H D-769 S CH2(3-F-Ph) H H OC2H5 HD-770 S CH2(4-F-Ph) H H OC2H5 H D-771 S CH2(2-OMe-Ph) H H OC2H5 H D-772S CH2(3-OMe-Ph) H H OC2H5 H D-773 S CH2(4-OMe-Ph) H H OC2H5 H D-774 SCH(CH3)Ph H H OC2H5 H D-775 S CH(CH3)(2-Cl-Ph) H H OC2H5 H D-776 SCH(CH3)(3-Cl-Ph) H H OC2H5 H D-777 S CH(CH3)(4-Cl-Ph) H H OC2H5 H D-778S CH(CH3)(2-CF3-Ph) H H OC2H5 H D-779 S CH(CH3)(3-CF3-Ph) H H OC2H5 HD-780 S CH(CH3)(4-CF3-Ph) H H OC2H5 H D-781 S Ph H H OC2H5 H D-782 S2-Cl-Ph H H OC2H5 H D-783 S 3-Cl-Ph H H OC2H5 H D-784 S 4-Cl-Ph H HOC2H5 H D-785 S 2-CF3-Ph H H OC2H5 H D-786 S 3-CF3-Ph H H OC2H5 H D-787S 4-CF3-Ph H H OC2H5 H D-788 S 2-CH3O-Ph H H OC2H5 H D-789 S 3-CH3O-Ph HH OC2H5 H D-790 S 4-CH3O-Ph H H OC2H5 H D-791 S 4-CF3O-Ph H H OC2H5 HD-792 S 4-CF3CH2O-Ph H H OC2H5 H D-793 S 4-PhO-Ph H H OC2H5 H D-794 S4-(4-Cl-Ph)O-Ph H H OC2H5 H D-795 S 4-(4-CF3-Ph)O-Ph H H OC2H5 H D-796 SOCH3 H H OC2H5 H D-797 S OC2H5 H H OC2H5 H D-798 S O-n-C3H7 H H OC2H5 HD-799 S O-i-C3H7 H H OC2H5 H D-800 S O-n-C4H9 H H OC2H5 H D-801 SO-i-C4H7 H H OC2H5 H D-802 S O-sec-C4H9 H H OC2H5 H D-803 S O-t-C4H9 H HOC2H5 H D-804 S O-n-C5H11 H H OC2H5 H D-805 S OCH2CH═CH2 H H OC2H5 HD-806 S OCH2C(CH3)═CH2 H H OC2H5 H D-807 S OCH2CH═CHCH3 H H OC2H5 HD-808 S OCH2CH═C(CH3)2 H H OC2H5 H D-809 S OCH2CCH H H OC2H5 H D-810 SOCH2CCCH3 H H OC2H5 H D-811 S OCH2Ph H H OC2H5 H D-812 S OCH(CH3)Ph H HOC2H5 H D-813 S OCH2(2-Cl-Ph) H H OC2H5 H D-814 S OCH2(3-Cl-Ph) H HOC2H5 H D-815 S OCH2(4-Cl-Ph) H H OC2H5 H D-816 S OCH2(2-OCH3-Ph) H HOC2H5 H D-817 S OCH2(3-OCH3-Ph) H H OC2H5 H D-818 S OCH2(4-OCH3-Ph) H HOC2H5 H D-819 S OCH2(2-CF3-Ph) H H OC2H5 H D-820 S OCH2(3-CF3-Ph) H HOC2H5 H D-821 S OCH2(4-CF3-Ph) H H OC2H5 H D-822 S OCH2(2-NO2-Ph) H HOC2H5 H D-823 S OCH2(3-NO2-Ph) H H OC2H5 H D-824 S OCH2(4-NO2-Ph) H HOC2H5 H D-825 O H H H H H D-826 O CH3 H H H H D-827 O C2H5 H H H H D-828O n-C3H7 H H H H D-829 O i-C3H7 H H H H D-830 O n-C4H9 H H H H D-831 Os-C4H9 H H H H D-832 O i-C4H9 H H H H D-833 O t-C4H9 H H H H D-834 OCH2Ph H H H H D-835 O Ph H H H H D-836 S H C2H5 H O D-837 S H i-C3H7 CH3NH D-838 S H CH3 CH3 NH

TABLE 5 Compounds of formula (Ie): (1e)

Compound U R^(2a) R^(e) E-1  N CH3 H E-2  N C2H5 H E-3  N n-C3H7 H E-4 N i-C3H7 H E-5  N n-C4H9 H E-6  N s-C4H9 H E-7  N i-C4H9 H E-8  N t-C4H9H E-9  N n-C5H11 H E-10 N n-C6H13 H E-11 N CH2CH═CH2 H E-12 NCH2C(CH3)═CH2 H E-13 N CH2C(CH3)═CHCH3 H E-14 N CH2CH═C(CH3)2 H E-15 NCH2CCl═CH2 H E-16 N CH2CH═CCl2 H E-17 N CH2CH═CHCF3 H E-18 N CH2CH═CHPhH E-19 N CH(CH3)CH═CH2 H E-20 N CH2CCH H E-21 N CH2CCCH3 H E-22 N CH2CF3H E-23 N CH2CH2OCH3 H E-24 N CH2CH2OC2H5 H E-25 N CH2CH2CH2OCH3 H E-26 NCH2CH2CH2OC2H5 H E-27 N CH2CH(OCH3)2 H E-28 N CH2CN H E-29 N CH2CO2H HE-30 N CH2CO2CH3 H E-31 N CH2CO2C2H5 H E-32 N CH(CH3)CO2CH3 H E-33 Ncyclo-C3H7 H E-34 N cyclo-C5H9 H E-35 N cyclo-C6H11 H E-36 NCH2(cyclo-C3H5) H E-37 N CH2(cyclo-C5H9) H E-38 N CH2(cyclo-C6H11) HE-39 N CH2Ph H E-40 N CH2(2-Cl-Ph) H E-41 N CH2(3-Cl-Ph) H E-42 NCH2(4-Cl-Ph) H E-43 N CH2(2-CF3-Ph) H E-44 N CH2(3-CF3-Ph) H E-45 NCH2(4-CF3-Ph) H E-46 N CH2(2-F-Ph) H E-47 N CH2(3-F-Ph) H E-48 NCH2(4-F-Ph) H E-49 N CH2(2-OMe-Ph) H E-50 N CH2(3-OMe-Ph) H E-51 NCH2(4-OMe-Ph) H E-52 N CH(CH3)Ph H E-53 N CH(CH3)(2-Cl-Ph) H E-54 NCH(CH3)(3-Cl-Ph) H E-55 N CH(CH3)(4-Cl-Ph) H E-56 N CH(CH3)(2-CF3-Ph) HE-57 N CH(CH3)(3-CF3-Ph) H E-58 N CH(CH3)(4-CF3-Ph) H E-59 N Ph H E-60 N2-Cl-Ph H E-61 N 3-Cl-Ph H E-62 N 4-Cl-Ph H E-63 N 2-CF3-Ph H E-64 N3-CF3-Ph H E-65 N 4-CF3-Ph H E-66 N 2-CH3O-Ph H E-67 N 3-CH3O-Ph H E-68N 4-CH3O-Ph H E-69 N 4-CF3O-Ph H E-70 N 4-CF3CH2O-Ph H E-71 N 4-PhO-Ph HE-72 N 4-(4-Cl-Ph)O-Ph H E-73 N 4-(4-CF3-Ph)O-Ph H E-74 CH CH3 H E-75 CHC2H5 H E-76 CH n-C3H7 H E-77 CH i-C3H7 H E-78 CH n-C4H9 H E-79 CH s-C4H9H E-80 CH i-C4H9 H E-81 CH t-C4H9 H E-82 CH n-C5H11 H E-83 CH n-C6H13 HE-84 CH CH2CH═CH2 H E-85 CH CH2O(CH3)═CH2 H E-86 CH CH2C(CH3)═CHCH3 HE-87 CH CH2CH═C(CH3)2 H E-88 CH CH2CCl═CH2 H E-89 CH CH2CH═CCl2 H E-90CH CH2CH═CHCF3 H E-91 CH CH2CH═CHPh H E-92 CH CH(CH3)CH═CH2 H E-93 CHCH2CCH H E-94 CH CH2CCCH3 H E-95 CH CH2CF3 H E-96 CH CH2CH2OCH3 H E-97CH CH2CH2CO2H5 H E-98 CH CH2CH2CH2OCH3 H E-99 CH CH2CH2CH2OC2H5 H E-100CH CH2CH(OCH3)2 H E-101 CH CH2CN H E-102 CH CH2CO2H H E-103 CH CH2CO2CH3H E-104 CH CH2CO2C2H5 H E-105 CH CH(CH3)CO2CH3 H E-106 CH cyclo-C3H7 HE-107 CH cyclo-C5H9 H E-108 CH cyclo-C6H11 H E-109 CH CH2(cyclo-C3H5) HE-110 CH CH2(cyclo-C5H9) H E-111 CH CH2(cyclo-C6H11) H E-112 CH CH2Ph HE-113 CH CH2(2-Cl-Ph) H E-114 CH CH2(3-Cl-Ph) H E-115 CH CH2(4-Cl-Ph) HE-116 CH CH2(2-CF3-Ph) H E-117 CH CH2(3-CF3-Ph) H E-118 CH CH2(4-CF3-Ph)H E-119 CH CH2(2-F-Ph) H E-120 CH CH2(3-F-Ph) H E-121 CH CH2(4-F-Ph) HE-122 CH CH2(2-OMe-Ph) H E-123 CH CH2(3-OMe-Ph) H E-124 CH CH2(4-OMe-Ph)H E-125 CH CH(CH3)Ph H E-126 CH CH(CH3)(2-Cl-Ph) H E-127 CHCH(CH3)(3-Cl-Ph) H E-128 CH CH(CH3)(4-Cl-Ph) H E-129 CHCH(CH3)(2-CF3-Ph) H E-130 CH CH(CH3)(3-CF3-Ph) H E-131 CHCH(CH3)(4-CF3-Ph) H E-132 CH Ph H E-133 CH 2-Cl-Ph H E-134 CH 3-Cl-Ph HE-135 CH 4-Cl-Ph H E-136 CH 2-CF3-Ph H E-137 CH 3-CF3-Ph H E-138 CH4-CF3-Ph H E-139 CH 2-CH3O-Ph H E-140 CH 3-CH3O-Ph H E-141 CH 4-CH3O-PhH E-142 CH 4-CF3O-Ph H E-143 CH 4-CF3CH2O-Ph H E-144 CH 4-PhO-Ph H E-145CH 4-(4-Cl-Ph)O-Ph H E-146 CH 4-(4-CF3-Ph)O-Ph H E-147 CH OCH3 H E-148CH OC2H5 H E-149 CH O-n-C3H7 H E-150 CH O-i-C3H7 H E-151 CH O-n-C4H9 HE-152 CH O-i-C4H7 H E-153 CH O-sec-C4H9 H E-154 CH O-t-C4H9 H E-155 CHO-n-C5H11 H E-156 CH OCH2CH═CH2 H E-157 CH OCH2C(CH3)═CH2 H E-158 CHOCH2CH═CHCH3 H E-159 CH OCH2CH═C(CH3)2 H E-160 CH OCH2CCH H E-161 CHOCH2CCCH3 H E-162 CH OCH2Ph H E-163 CH OCH(CH3)Ph H E-164 CHOCH2(2-Cl-Ph) H E-165 CH OCH2(3-Cl-Ph) H E-166 CH OCH2(4-Cl-Ph) H E-167CH OCH2(2-OCH3-Ph) H E-168 CH OCH2(3-OCH3-Ph) H E-169 CH OCH2(4-OCH3-Ph)H E-170 CH OCH2(2-CF3-Ph) H E-171 CH OCH2(3-CF3-Ph) H E-172 CHOCH2(4-CF3-Ph) H E-173 CH OCH2(2-NO2-Ph) H E-174 CH OCH2(3-NO2-Ph) HE-175 CH OCH2(4-NO2-Ph) H E-176 N CH3 CH3 E-177 N C2H5 CH3 E-178 Nn-C3H7 CH3 E-179 N i-C3H7 CH3 E-180 N n-C4H9 CH3 E-181 N s-C4H9 CH3E-182 N i-C4H9 CH3 E-183 N t-C4H9 CH3 E-184 N n-C5H11 CH3 E-185 Nn-C6H13 CH3 E-186 N CH2CH═CH2 CH3 E-187 N CH2C(CH3)═CH2 CH3 E-188 NCH2C(CH3)═CHCH3 CH3 E-189 N CH2CH═C(CH3)2 CH3 E-190 N CH2CCl═CH2 CH3E-191 N CH2CH═CCl2 CH3 E-192 N CH2CH═CHCF3 CH3 E-193 N CH2CH═CHPh CH3E-194 N CH(CH3)CH═CH2 CH3 E-195 N CH2CCH CH3 E-196 N CH2CCCH3 CH3 E-197N CH2CF3 CH3 E-198 N CH2CH2OCH3 CH3 E-199 N CH2CH2OC2H5 CH3 E-200 NCH2CH2CH2OCH3 CH3 E-201 N CH2CH2CH2OC2H5 CH3 E-202 N CH2CH(OCH3)2 CH3E-203 N CH2CN CH3 E-204 N CH2CO2H CH3 E-205 N CH2CO2CH3 CH3 E-206 NCH2CO2C2H5 CH3 E-207 N CH(CH3)CO2CH3 CH3 E-208 N cyclo-C3H7 CH3 E-209 Ncyclo-C5H9 CH3 E-210 N cyclo-C6H11 CH3 E-211 N CH2(cyclo-C3H5) CH3 E-212N CH2(cyclo-C5H9) CH3 E-213 N CH2(cyclo-C6H11) CH3 E-214 N CH2Ph CH3E-215 N CH2(2-Cl-Ph) CH3 E-216 N CH2(3-Cl-Ph) CH3 E-217 N CH2(4-Cl-Ph)CH3 E-218 N CH2(2-CF3-Ph) CH3 E-219 N CH2(3-CF3-Ph) CH3 E-220 NCH2(4-CF3-Ph) CH3 E-221 N CH2(2-F-Ph) CH3 E-222 N CH2(3-F-Ph) CH3 E-223N CH2(4-F-Ph) CH3 E-224 N CH2(2-OMe-Ph) CH3 E-225 N CH2(3-OMe-Ph) CH3E-226 N CH2(4-OMe-Ph) CH3 E-227 N CH(CH3)Ph CH3 E-228 N CH(CH3)(2-Cl-Ph)CH3 E-229 N CH(CH3)(3-Cl-Ph) CH3 E-230 N CH(CH3)(4-Cl-Ph) CH3 E-231 NCH(CH3)(2-CF3-Ph) CH3 E-232 N CH(CH3)(3-CF3-Ph) CH3 E-233 NCH(CH3)(4-CF3-Ph) CH3 E-234 N Ph CH3 E-235 N 2-Cl-Ph CH3 E-236 N 3-Cl-PhCH3 E-237 N 4-Cl-Ph CH3 E-238 N 2-CF3-Ph CH3 E-239 N 3-CF3-Ph CH3 E-240N 4-CF3-Ph CH3 E-241 N 2-CH3O-Ph CH3 E-242 N 3-CH3O-Ph CH3 E-243 N4-CH3O-Ph CH3 E-244 N 4-CF3O-Ph CH3 E-245 N 4-CF3CH2O-Ph CH3 E-246 N4-PhO-Ph CH3 E-247 N 4-(4-Cl-Ph)O-Ph CH3 E-248 N 4-(4-CF3-Ph)O-Ph CH3E-249 CH CH3 CH3 E-250 CH C2H5 CH3 E-251 CH n-C3H7 CH3 E-252 CH i-C3H7CH3 E-253 CH n-C4H9 CH3 E-254 CH s-C4H9 CH3 E-255 CH i-C4H9 CH3 E-256 CHt-C4H9 CH3 E-257 CH n-C5H11 CH3 E-258 CH n-C6H13 CH3 E-259 CH CH2CH═CH2CH3 E-260 CH CH2C(CH3)═CH2 CH3 E-261 CH CH2C(CH3)═CHCH3 CH3 E-262 CHCH2CH═C(CH3)2 CH3 E-263 CH CH2CCl═CH2 CH3 E-264 CH CH2CH═CCl2 CH3 E-265CH CH2CH═CHCF3 CH3 E-266 CH CH2CH═CHPh CH3 E-267 CH CH(CH3)CH═CH2 CH3E-268 CH CH2OCH CH3 E-269 CH CH2CCCH3 CH3 E-270 CH CH2CF3 CH3 E-271 CHCH2CH2OCH3 CH3 E-272 CH CH2CH2OC2H5 CH3 E-273 CH CH2CH2CH2OCH3 CH3 E-274CH CH2CH2CH2OC2H5 CH3 E-275 CH CH2CH(OCH3)2 CH3 E-276 CH CH2CN CH3 E-277CH CH2CO2H CH3 E-278 CH CH2CO2CH3 CH3 E-279 CH CH2CO2C2H5 CH3 E-280 CHCH(CH3)CO2CH3 CH3 E-281 CH cyclo-C3H7 CH3 E-282 CH cyclo-C5H9 CH3 E-283CH cyclo-C6H11 CH3 E-284 CH CH2(cyclo-C3H5) CH3 E-285 CH CH2(cyclo-C5H9)CH3 E-286 CH CH2(cyclo-C6H11) CH3 E-287 CH CH2Ph CH3 E-288 CHCH2(2-Cl-Ph) CH3 E-289 CH CH2(3-Cl-Ph) CH3 E-290 CH CH2(4-Cl-Ph) CH3E-291 CH CH2(2-CF3-Ph) CH3 E-292 CH CH2(3-CF3-Ph) CH3 E-293 CHCH2(4-CF3-Ph) CH3 E-294 CH CH2(2-F-Ph) CH3 E-295 CH CH2(3-F-Ph) CH3E-296 CH CH2(4-F-Ph) CH3 E-297 CH CH2(2-OMe-Ph) CH3 E-298 CHCH2(3-OMe-Ph) CH3 E-299 CH CH2(4-OMe-Ph) CH3 E-300 CH CH(CH3)Ph CH3E-301 CH CH(CH3)(2-Cl-Ph) CH3 E-302 CH CH(CH3)(3-Cl-Ph) CH3 E-303 CHCH(CH3)(4-Cl-Ph) CH3 E-304 CH CH(CH3)(2-CF3-Ph) CH3 E-305 CHCH(CH3)(3-CF3-Ph) CH3 E-306 CH CH(CH3)(4-CF3-Ph) CH3 E-307 CH Ph CH3E-308 CH 2-Cl-Ph CH3 E-309 CH 3-Cl-Ph CH3 E-310 CH 4-Cl-Ph CH3 E-311 CH2-CF3-Ph CH3 E-312 CH 3-CF3-Ph CH3 E-313 CH 4-CF3-Ph CH3 E-314 CH2-CH3O-Ph CH3 E-315 CH 3-CH3O-Ph CH3 E-316 CH 4-CH3O-Ph CH3 E-317 CH4-CF3O-Ph CH3 E-318 CH 4-CF3CH2O-Ph CH3 E-319 CH 4-PhO-Ph CH3 E-320 CH4-(4-Cl-Ph)O-Ph CH3 E-321 CH 4-(4-CF3-Ph)O-Ph CH3 E-322 CH OCH3 CH3E-323 CH OC2H5 CH3 E-324 CH O-n-C3H7 CH3 E-325 CH O-i-C3H7 CH3 E-326 CHO-n-C4H9 CH3 E-327 CH O-i-C4H7 CH3 E-328 CH O-sec-C4H9 CH3 E-329 CHO-t-C4H9 CH3 E-330 CH O-n-C5H11 CH3 E-331 CH OCH2CH═CH2 CH3 E-332 CHOCH2C(CH3)═CH2 CH3 E-333 CH OCH2CH═CHCH3 CH3 E-334 CH OCH2CH═C(CH3)2 CH3E-335 CH OCH2OCH CH3 E-336 CH OCH2CCCH3 CH3 E-337 CH OCH2Ph CH3 E-338 CHOCH(CH3)Ph CH3 E-339 CH OCH2(2-Cl-Ph) CH3 E-340 CH OCH2(3-Cl-Ph) CH3E-341 CH OCH2(4-Cl-Ph) CH3 E-342 CH OCH2(2-OCH3-Ph) CH3 E-343 CHOCH2(3-OCH3-Ph) CH3 E-344 CH OCH2(4-OCH3-Ph) CH3 E-345 CH OCH2(2-CF3-Ph)CH3 E-346 CH OCH2(3-CF3-Ph) CH3 E-347 CH OCH2(4-CF3-Ph) CH3 E-348 CHOCH2(2-NO2-Ph) CH3 E-349 CH OCH2(3-NO2-Ph) CH3 E-350 CH OCH2(4-NO2-Ph)CH3 E-351 CH CH3 Ph E-352 CH C2H5 Ph E-353 CH n-C3H7 Ph E-354 CH i-C3H7Ph E-355 CH n-C4H9 Ph E-356 CH s-C4H9 Ph E-357 CH i-C4H9 Ph E-358 CHt-C4H9 Ph E-359 CH n-C5H11 Ph E-360 CH n-C6H13 Ph E-361 CH CH2CH═CH2 PhE-362 CH CH2C(CH3)═CH2 Ph E-363 CH CH2C(CH3)═CHCH3 Ph E-364 CHCH2CH═C(CH3)2 Ph E-365 CH CH2CCl═CH2 Ph E-366 CH CH2CH═CCl2 Ph E-367 CHCH2CH═CHCF3 Ph E-368 CH CH2CH═CHPh Ph E-369 CH CH(CH3)CH═CH2 Ph E-370 CHCH2CCH Ph E-371 CH CH2CCCH3 Ph E-372 CH CH2CF3 Ph E-373 CH CH2CH2OCH3 PhE-374 CH CH2CH2OC2H5 Ph E-375 CH CH2CH2CH2OCH3 Ph E-376 CHCH2CH2CH2OC2H5 Ph E-377 CH CH2CH(OCH3)2 Ph E-378 CH CH2CN Ph E-379 CHCH2CO2H Ph E-380 CH CH2CO2CH3 Ph E-381 CH CH2CO2C2H5 Ph E-382 CHCH(CH3)CO2CH3 Ph E-383 CH cyclo-C3H7 Ph E-384 CH cyclo-C5H9 Ph E-385 CHcyclo-C6H11 Ph E-386 CH CH2(cyclo-C3H5) Ph E-387 CH CH2(cyclo-C5H9) PhE-388 CH CH2(cyclo-C6H11) Ph E-389 CH CH2Ph Ph E-390 CH CH2(2-Cl-Ph) PhE-391 CH CH2(3-Cl-Ph) Ph E-392 CH CH2(4-Cl-Ph) Ph E-393 CH CH2(2-CF3-Ph)Ph E-394 CH CH2(3-CF3-Ph) Ph E-395 CH CH2(4-CF3-Ph) Ph E-396 CHCH2(2-F-Ph) Ph E-397 CH CH2(3-F-Ph) Ph E-398 CH CH2(4-F-Ph) Ph E-399 CHCH2(2-OMe-Ph) Ph E-400 CH CH2(3-OMe-Ph) Ph E-401 CH CH2(4-OMe-Ph) PhE-402 CH CH(CH3)Ph Ph E-403 CH CH(CH3)(2-Cl-Ph) Ph E-404 CHCH(CH3)(3-Cl-Ph) Ph E-405 CH CH(CH3)(4-Cl-Ph) Ph E-406 CHCH(CH3)(2-CF3-Ph) Ph E-407 CH CH(CH3)(3-CF3-Ph) Ph E-408 CHCH(CH3)(4-CF3-Ph) Ph E-409 CH Ph Ph E-410 CH 2-Cl-Ph Ph E-411 CH 3-Cl-PhPh E-412 CH 4-Cl-Ph Ph E-413 CH 2-CF3-Ph Ph E-414 CH 3-CF3-Ph Ph E-415CH 4-CF3-Ph Ph E-416 CH 2-CH3O-Ph Ph E-417 CH 3-CH3O-Ph Ph E-418 CH4-CH3O-Ph Ph E-419 CH 4-CF3O-Ph Ph E-420 CH 4-CF3CH2O-Ph Ph E-421 CH4-PhO-Ph Ph E-422 CH 4-(4-Cl-Ph)O-Ph Ph E-423 CH 4-(4-CF3-Ph)O-Ph PhE-424 CH OCH3 Ph E-425 CH OC2H5 Ph E-426 CH O-n-C3H7 Ph E-427 CHO-i-C3H7 Ph E-428 CH O-n-C4H9 Ph E-429 CH O-i-C4H7 Ph E-430 CHO-sec-C4H9 Ph E-431 CH O-t-C4H9 Ph E-432 CH O-n-C5H11 Ph E-433 CHOCH2CH═CH2 Ph E-434 CH OCH2C(CH3)═CH2 Ph E-435 CH OCH2CH═CHCH3 Ph E-436CH OCH2CH═C(CH3)2 Ph E-437 CH OCH2CCH Ph E-438 CH OCH2CCCH3 Ph E-439 CHOCH2Ph Ph E-440 CH OCH(CH3)Ph Ph E-441 CH OCH2(2-Cl-Ph) Ph E-442 CHOCH2(3-Cl-Ph) Ph E-443 CH OCH2(4-Cl-Ph) Ph E-444 CH OCH2(2-OCH3-Ph) PhE-445 CH OCH2(3-OCH3-Ph) Ph E-446 CH OCH2(4-OCH3-Ph) Ph E-447 CHOCH2(2-CF3-Ph) Ph E-448 CH OCH2(3-CF3-Ph) Ph E-449 CH OCH2(4-CF3-Ph) PhE-450 CH OCH2(2-NO2-Ph) Ph E-451 CH OCH2(3-NO2-Ph) Ph E-452 CHOCH2(4-NO2-Ph) Ph E-453 N CH3 Ph E-454 N C2H5 Ph E-455 N n-C3H7 Ph E-456N i-C3H7 Ph E-457 N n-C4H9 Ph E-458 N s-C4H9 Ph E-459 N i-C4H9 Ph E-460N t-C4H9 Ph E-461 N n-C5H11 Ph E-462 N n-C6H13 Ph E-463 N CH2CH═CH2 PhE-464 N CH2C(CH3)═CH2 Ph E-465 N CH2C(CH3)═CHCH3 Ph E-466 NCH2CH═C(CH3)2 Ph E-467 N CH2CCl═CH2 Ph E-468 N CH2CH═CCl2 Ph E-469 NCH2CH═CHCF3 Ph E-470 N CH2CH═CHPh Ph E-471 N CH(CH3)CH═CH2 Ph E-472 NCH2CCH Ph E-473 N CH2CCCH3 Ph E-474 N CH2CF3 Ph E-475 N CH2CH2OCH3 PhE-476 N CH2CH2OC2H5 Ph E-477 N CH2CH2CH2OCH3 Ph E-478 N CH2CH2CH2OC2H5Ph E-479 N CH2CH(OCH3)2 Ph E-480 N CH2CN Ph E-481 N CH2CO2H Ph E-482 NCH2CO2CH3 Ph E-483 N CH2CO2C2H5 Ph E-484 N CH(CH3)CO2CH3 Ph E-485 Ncyclo-C3H7 Ph E-486 N cyclo-C5H9 Ph E-487 N cyclo-C6H11 Ph E-488 NCH2(cyclo-C3H5) Ph E-489 N CH2(cyclo-C5H9) Ph E-490 N CH2(cyclo-C6H11)Ph E-491 N CH2Ph Ph E-492 N CH2(2-Cl-Ph) Ph E-493 N CH2(3-Cl-Ph) PhE-494 N CH2(4-Cl-Ph) Ph E-495 N CH2(2-CF3-Ph) Ph E-496 N CH2(3-CF3-Ph)Ph E-497 N CH2(4-CF3-Ph) Ph E-498 N CH2(2-F-Ph) Ph E-499 N CH2(3-F-Ph)Ph E-500 N CH2(4-F-Ph) Ph E-501 N CH2(2-OMe-Ph) Ph E-502 N CH2(3-OMe-Ph)Ph E-503 N CH2(4-OMe-Ph) Ph E-504 N CH(CH3)Ph Ph E-505 NCH(CH3)(2-Cl-Ph) Ph E-506 N CH(CH3)(3-Cl-Ph) Ph E-507 N CH(CH3)(4-Cl-Ph)Ph E-508 N CH(CH3)(2-CF3-Ph) Ph E-509 N CH(CH3)(3-CF3-Ph) Ph E-510 NCH(CH3)(4-CF3-Ph) Ph E-511 N Ph Ph E-512 N 2-Cl-Ph Ph E-513 N 3-Cl-Ph PhE-514 N 4-Cl-Ph Ph E-515 N 2-CF3-Ph Ph E-516 N 3-CF3-Ph Ph E-517 N4-CF3-Ph Ph E-518 N 2-CH3O-Ph Ph E-519 N 3-CH3O-Ph Ph E-520 N 4-CH3O-PhPh E-521 N 4-CF3O-Ph Ph E-522 N 4-CF3CH2O-Ph Ph E-523 N 4-PhO-Ph PhE-524 N 4-(4-Cl-Ph)O-Ph Ph E-525 N 4-(4-CF3-Ph)O-Ph Ph E-526 CH CH3 CF3E-527 CH i-C3H7 CF3 E-528 CH CH2CHCH2 CF3 E-529 CH CH2Ph CF3 E-530 CH PhCF3 E-531 CH 3-CF3-Ph CF3 E-532 N CH3 CF3 E-533 N i-C3H7 CF3 E-534 NCH2CHCH2 CF3 E-535 N CH2Ph CF3 E-536 N Ph CF3 E-537 N 3-CF3-Ph CF3

TABLE 6 Compounds of formula (If) wherein t is 0 or 1. Compounds F-1 toF-78 represent individual compounds in which t is 0, whilst compoundsG-1 to G-78 represent individual compounds in which t is 1. (1f)

Compound R² R^(f) F-1  G-1  H H F-2  G-2  CH3 H F-3  G-3  C2H5 H F-4 G-4  n-C3H7 H F-5  G-5  i-C3H7 H F-6  G-6  n-C4H9 H F-7  G-7  s-C4H9 HF-8  G-8  i-C4H9 H F-9  G-9  t-C4H9 H F-10 G-10 n-C5H11 H F-11 G-11n-C6H13 H F-12 G-12 CH2CH═CH2 H F-13 G-13 CH2C(CH3)═CH2 H F-14 G-14CH2C(CH3)═CHCH3 H F-15 G-15 CH2CH═C(CH3)2 H F-16 G-16 CH2CCl═CH2 H F-17G-17 CH2CH═CCl2 H F-18 G-18 CH2CH═CHCF3 H F-19 G-19 CH2CH═CHPh H F-20G-20 CH(CH3)CH═CH2 H F-21 G-21 CH2CCH H F-22 G-22 CH2CCCH3 H F-23 G-23CH2CF3 H F-24 G-24 CH2CH2OCH3 H F-25 G-25 CH2CH2OC2H5 H F-26 G-26CH2CH2CH2OCH3 H F-27 G-27 CH2CH2CH2OC2H5 H F-28 G-28 CH2CH(OCH3)2 H F-29G-29 CH2CN H F-30 G-30 CH2CO2CH3 H F-31 G-31 CH2CO2C2H5 H F-32 G-32CH(CH3)CO2CH3 H F-33 G-33 cyclo-C3H7 H F-34 G-34 cyclo-C5H9 H F-35 G-35cyclo-C6H11 H F-36 G-36 CH2(cyclo-C3H5) H F-37 G-37 CH2(cyclo-C5H9) HF-38 G-38 CH2(cyclo-C6H11) H F-39 G-39 CH2Ph H F-40 G-40 CH2(2-Cl-Ph) HF-41 G-41 CH2(3-Cl-Ph) H F-42 G-42 CH2(4-Cl-Ph) H F-43 G-43CH2(2-CF3-Ph) H F-44 G-44 CH2(3-CF3-Ph) H F-45 G-45 CH2(4-CF3-Ph) H F-46G-46 CH2(2-F-Ph) H F-47 G-47 CH2(3-F-Ph) H F-48 G-48 CH2(4-F-Ph) H F-49G-49 CH2(2-OMe-Ph) H F-50 G-50 CH2(3-OMe-Ph) H F-51 G-51 CH2(4-OMe-Ph) HF-52 G-52 CH(CH3)Ph H F-53 G-53 CH(CH3)(2-Cl-Ph) H F-54 G-54CH(CH3)(3-Cl-Ph) H F-55 G-55 CH(CH3)(4-Cl-Ph) H F-56 G-56CH(CH3)(2-CF3-Ph) H F-57 G-57 CH(CH3)(3-CF3-Ph) H F-58 G-58CH(CH3)(4-CF3-Ph) H F-59 G-59 H 4-Cl F-60 G-60 CH3 4-Cl F-61 G-61CH2CH═CH2 4-Cl F-62 G-62 CH2C(CH3)═CH2 4-Cl F-63 G-63 CH2Ph 4-Cl F-64G-64 H 5-Cl F-65 G-65 CH3 5-Cl F-66 G-66 CH2CH═CH2 5-Cl F-67 G-67CH2C(CH3)═CH2 5-Cl F-68 G-68 CH2Ph 5-Cl F-69 G-69 H 6-Cl F-70 G-70 CH36-Cl F-71 G-71 CH2CH═CH2 6-Cl F-72 G-72 CH2C(CH3)═CH2 6-Cl F-73 G-73CH2Ph 6-Cl F-74 G-74 H 7-Cl F-75 G-75 CH3 7-Cl F-76 G-76 CH2CH═CH2 7-ClF-77 G-77 CH2C(CH3)═CH2 7-Cl F-78 G-78 CH2Ph 7-Cl

TABLE 7 Compounds of formula (Ig). Compounds H-1 to H-102 representindividual compounds in which Y is S and V is CH₂; compounds I-1 toI-102 represent individual compounds in which Y is S and V is O;compounds J-1 to J-102 represent individual compounds in which Y is Oand V is CH₂. (1g)

Compound R² R^(g) H-1  I-1  J-1  H H H-2  I-2  J-2  CH3 H H-3  I-3  J-3 C2H5 H H-4  I-4  J-4  n-C3H7 H H-5  I-5  J-5  i-C3H7 H H-6  I-6  J-6 n-C4H9 H H-7  I-7  J-7  s-C4H9 H H-8  I-8  J-8  i-C4H9 H H-9  I-9  J-9 t-C4H9 H H-10 I-10 J-10 n-C5H11 H H-11 I-11 J-11 n-C6H13 H H-12 I-12J-12 CH2CH═CH2 H H-13 I-13 J-13 CH2C(CH3)═CH2 H H-14 I-14 J-14CH2C(CH3)═CHCH3 H H-15 I-15 J-15 CH2CH═C(CH3)2 H H-16 I-16 J-16CH2CCl═CH2 H H-17 I-17 J-17 CH2CH═CCl2 H H-18 I-18 J-18 CH2CH═CHCF3 HH-19 I-19 J-19 CH2CH═CHPh H H-20 I-20 J-20 CH(CH3)CH═CH2 H H-21 I-21J-21 CH2CCH H H-22 I-22 J-22 CH2CCCH3 H H-23 I-23 J-23 CH2CF3 H H-24I-24 J-24 CH2CH2OCH3 H H-25 I-25 J-25 CH2CH2OC2H5 H H-26 I-26 J-26CH2CH2CH2OCH3 H H-27 I-27 J-27 CH2CH2CH2OC2H5 H H-28 I-28 J-28CH2CH(OCH3)2 H H-29 I-29 J-29 CH2CN H H-30 I-30 J-30 CH2CO2CH3 H H-31I-31 J-31 CH2CO2C2H5 H H-32 I-32 J-32 CH(CH3)CO2CH3 H H-33 I-33 J-33cyclo-C3H7 H H-34 I-34 J-34 cyclo-C5H9 H H-35 I-35 J-35 cyclo-C6H11 HH-36 I-36 J-36 CH2(cyclo-C3H5) H H-37 I-37 J-37 CH2(cyclo-C5H9) H H-38I-38 J-38 CH2(cyclo-C6H11) H H-39 I-39 J-39 CH2Ph H H-40 I-40 J-40CH2(2-Cl-Ph) H H-41 I-41 J-41 CH2(3-Cl-Ph) H H-42 I-42 J-42 CH2(4-Cl-Ph)H H-43 I-43 J-43 CH2(2-CF3-Ph) H H-44 I-44 J-44 CH2(3-CF3-Ph) H H-45I-45 J-45 CH2(4-CF3-Ph) H H-46 I-46 J-46 CH2(2-F-Ph) H H-47 I-47 J-47CH2(3-F-Ph) H H-48 I-48 J-48 CH2(4-F-Ph) H H-49 I-49 J-49 CH2(2-OMe-Ph)H H-50 I-50 J-50 CH2(3-OMe-Ph) H H-51 I-51 J-51 CH2(4-OMe-Ph) H H-52I-52 J-52 CH(CH3)Ph H H-53 I-53 J-53 CH(CH3)(2-Cl-Ph) H H-54 I-54 J-54CH(CH3)(3-Cl-Ph) H H-55 I-55 J-55 CH(CH3)(4-Cl-Ph) H H-56 I-56 J-56CH(CH3)(2-CF3-Ph) H H-57 I-57 J-57 CH(CH3)(3-CF3-Ph) H H-58 I-58 J-58CH(CH3)(4-CF3-Ph) H H-59 I-59 J-59 Ph H H-60 I-60 J-60 2-Cl-Ph H H-61I-61 J-61 3-Cl-Ph H H-62 I-62 J-62 4-Cl-Ph H H-63 I-63 J-63 2-CF3-Ph HH-64 I-64 J-64 3-CF3-Ph H H-65 I-65 J-65 4-CF3-Ph H H-66 I-66 J-662-CH3O-Ph H H-67 I-67 J-67 3-CH3O-Ph H H-68 I-68 J-68 4-CH3O-Ph H H-69I-69 J-69 4-CF3O-Ph H H-70 I-70 J-70 4-CF3CH2O-Ph H H-71 I-71 J-714-PhO-Ph H H-72 I-72 J-72 4-(4-Cl-Ph)O-Ph H H-73 I-73 J-734-(4-CF3-Ph)O-Ph H H-74 I-74 J-74 OCH3 H H-75 I-75 J-75 OC2H5 H H-76I-76 J-76 O-n-C3H7 H H-77 I-77 J-77 O-i-C3H7 H H-78 I-78 J-78 O-n-C4H9 HH-79 I-79 J-79 O-i-C4H7 H H-80 I-80 J-80 O-sec-C4H9 H H-81 I-81 J-81O-t-C4H9 H H-82 I-82 J-82 O-n-C5H11 H H-83 I-83 J-83 OCH2CH═CH2 H H-84I-84 J-84 OCH2C(CH3)═CH2 H H-85 I-85 J-85 OCH2CH═CHCH3 H H-86 I-86 J-86OCH2CH═C(CH3)2 H H-87 I-87 J-87 OCH2CCH H H-88 I-88 J-88 OCH2CCCH3 HH-89 I-89 J-89 OCH2Ph H H-90 I-90 J-90 OCH(CH3)Ph H H-91 I-91 J-91OCH2(2-Cl-Ph) H H-92 I-92 J-92 OCH2(3-Cl-Ph) H H-93 I-93 J-93OCH2(4-Cl-Ph) H H-94 I-94 J-94 OCH2(2-OCH3-Ph) H H-95 I-95 J-95OCH2(3-OCH3-Ph) H H-96 I-96 J-96 OCH2(4-OCH3-Ph) H H-97 I-97 J-97OCH2(2-CF3-Ph) H H-98 I-98 J-98 OCH2(3-CF3-Ph) H H-99 I-99 J-99OCH2(4-CF3-Ph) H  H-100  I-100  J-100 OCH2(2-NO2-Ph) H  H-101  I-101 J-101 OCH2(3-NO2-Ph) H  H-102  I-102  J-102 OCH2(4-NO2-Ph) H

TABLE 8 Compounds of formula (Ih): (Ih)

Compound R^(h) R^(j) K-1 H H K-2 CH3 H K-3 H CH3 K-4 CH3 CH3

TABLE 9 Compounds of formula (Ii); (Ii)

Compound R^(j) L-1 H

TABLE 10 1H-NMR spectral details for representative Examples from theabove Tables. Spectra were measured in deuterochloroform unlessotherwise stated. Cpd 1H-NMR A-1 11.24(1H, s) 9.20(1H, s) 8.80(1H, d)7.57(1H, d) 3.08(3H, d) 2.53(3H, s) A-11 11.04(1H, s) 9.18(1H, s)8.79(1H, d) 7.57(1H, d) 5.93(1H, m) 5.26(1H, d) 5.20(1H, d) 3.86(2H, d)3.08(3H, d) A-20 11.02(1H, s) 9.26(1H, s) 8.81(1H, d) 7.58(1H, d)3.97(2H, s) 3.09(3H, d) A-32 11.03(1H, s) 9.13(1H, s) 8.79(1H, d)7.57(1H, d) 7.25–7.40(5H) 4.44(2H, s) 3.05(3H, d) A-53 9.14(1H, s)8.78(1H, d) 7.58(1H, d) 3.29(6H, s) 2.55(2H, s) A-54 9.12(1H, s)8.75(1H, d) 7.56(1H, d) 3.15(6H, s) 3.11(2H, q) 1.34(3H, t) A-569.13(1H, s) 8.76(1H, d) 7.57(1H, d) 3.84(1H, m) 3.26(6H, s) 1.39(3H, d)A-59 9.14(1H, s) 8.76(1H, d) 7.57(1H, d) 3.29(6H, s) 3.00(2H, d)1.78(1H, m) 1.01(6H, d) A-67 9.15(1H, s) 8.76(1H, d) 7.57(1H, d)5.88(1H, m) 5.28(1H, d) 5.18(1H, d) 3.75(2H, d) 3.28(6H, s) A-729.23(1H, s) 8.77(1H, d) 7.57(1H, d) 3.86(1H, d) 3.28(6H, s) 2.28(1H, t)A-84 9.14(1H, s) 8.77(1H, d) 7.57(1H, d) 3.87(2H, s) 3.66(2H, s)3.29(6H, s) A-89 9.13(1H, s) 8.74(1H, d) 7.57(1H, d) 7.20–7.35(5H)4.35(2H, s) 3.28(6H, s) A-94 9.13(1H, s) 8.88(1H, d) 7.35–7.70(5H)4.37(2H, s) 3.29(6H, s) A-95 9.14(1H, s) 8.85(1H, d) 7.56(1H, d)7.50(2H, d) 7.28(2H, d) 4.37(2H, s) 3.29(6H, s) A-102 9.09(1H, s)8.76(1H, d) 7.58(1H, d) 7.40–7.25(5H) 4.93(1H, q) 3.24(6H, s) 1.75(3H,d) A-221 10.99(1H, s) 9.17(1H, s) 8.78(1H, d) 7.56(1H, d) 3.96(1H, m)3.14(2H, t) 1.75(2H, m) 1.33(6H, d) 1.00(3H, t) A-229 10.99(1H) 9.17(1H,s) 8.79(1H, d) 7.57(1H, d) 5.94(1H, m) 5.25(1H, d) 5.20(1H, d) 3.94(1H,m) 3.84(2H, d) 1.34(6H, d) A-230 10.99(1H) 9.15(1H, s) 8.78(1H, d)7.56(1H, d) 4.98(1H, s) 4.90(1H, s) 3.98(1H, m) 3.89(2H, s) 1.82(3H, s)1.34(6H, d) A-231 10.96(1H) 9.16(1H, s) 8.77(1H, d) 7.55(1H, d) 5.67(1H,m) 5.51(1H, m) 3.92(1H, m) 3.78(2H, d) 1.67(3H, d) 1.32(6H, d) A-23710.97(1H) 9.17(1H, s) 8.78(1H, d) 7.57(1H, d) 6.00(1H, m) 5.22(1H, d)5.13(1H, d) 4.68(1H, m) 3.94(1H, m) 1.50(3H, d) 1.33(6H, d) A-2509.13(1H, s) 8.78(1H, d) 7.57(1H, d) 7.20–7.35(5H) 4.43(2H, s) 3.91(1H,m) 1.35(6H, d) A-255 11.00(1H) 9.10(1H, s) 8.80(1H, d) 7.30–7.60(5H)4.46(2H, s) 3.90(1H, m) 1.35(6H, d) A-437 11.18(1H, s) 9.16(1H, s)8.79(1H, d) 7.57(1H, d) 6.0–5.8(1H, m) 5.3–5.0(2H, m) 3.84(2H, m)3.22(2H, t) 2.1–1.9(1H, m) 1.02(6H, d) A-438 11.19(1H, s) 9.15(1H, s)8.78(1H, d) 7.57(1H, d) 4.98(1H, s) 4.90(1H, s) 3.90(1H, s) 3.24(2H, t)2.1–1.9(1H, m) 1.82(3H, s) 1.03(6H, d) A-439 11.17(1H, s) 9.17(1H, s)8.78(1H, d) 7.57(1H, d) 5.8–5.4(2H, m) 3.80(2H, d) 3.20(2H, t)2.1–1.8(1H, m) 1.8–1.6(3H, m) 1.02(6H, d) A-458 1.17(1H, s) 9.12(1H, s)8.78(1H, d) 7.57(1H, d) 7.4–7.1(5H, m) 4.43(2H, s) 3.20(2H, t)2.1–1.9(1H, m) 1.01(6H, d) A-460 11.17(1H, s) 9.08(1H, s) 8.79(1H, d)7.57(1H, d) 7.4–7.1(4H, m) 4.38(2H, s) 3.21(2H, t) 2.1–1.9(1H, m)1.01(6H, d) A-479 11.50(1H) 9.15(1H, s) 8.89(1H, d) 7.57(1H, d) 2.52(3H,s) 1.53(9H, s) A-481 11.53(1H) 9.12((1H, s) 8.76(1H, d) 7.55(1H, d)3.15(2H, t) 1.71(2H, m) 1.52(9H, s) 0.99(3H, t) A-489 11.56(1H) 9.14(1H,s) 8.80(1H, d) 7.58(1H, d) 5.95(1H, m) 5.28(1H, d) 5.18(1H, d) 3.88(2H,d) 1.56(9H, s) A-490 11.53(1H) 9.10(1H, s) 8.76(1H, d) 7.55(1H, d)4.97(1H, s) 4.90(1H, s) 3.89(2H, s) 1.82(3H, s) 1.52(9H, s) A-49111.51(1H) 9.13(1H, s) 8.77(1H, d) 7.56(1H, d) 5.66(1H, m) 5.54(1H, m)3.80(2H) 1.64(3H, s) 1.52(9H, s) A-504 11.51(1H) 9.03(1H, s) 8.78(1H, d)7.56(1H, d) 3.91(2H, s) 3.65(3H, s) 1.56(9H, s) A-576 9.15(1H, s)8.77(1H, d) 7.57(1H, d) 5.85(1H, m) 5.28(1H, d) 5.19(1H, d) 3.73(2H, d)3.66(2H, q) 3.54(2H, t) 1.72(2H, d) 1.30(3H, t) 0.96(3H, t) A-71411.35(1H) 9.21(1H, s) 8.78(1H, d) 7.57(1H, d) 7.25–7.45(5H) 4.60(2H, d)2.53(3H, s) A-715 11.37(1H, s) 9.20(1H, s) 8.79(1H, d) 7.57(1H, d)7.23–7.43(5H) 4.29(2H, d) 3.19(2H, q) 1.35(3H, t) A-717 11.38(1H)9.20(1H, s) 8.78(1H, d) 7.57(1H, d) 7.25–7.42(5H) 4.56(2H, s) 4.12(1H,m) 1.40(6H, d) A-724 11.36(1H, s) 9.15(1H, s)8.78(1H, d) 7.58(1H, d)7.25–7.45(5H) 5.93(1H, m) 5.24(1H, d)5.14(1H, d)4.57(2H, d) 3.87(2H, d)A-733 11.32(1H) 9.27(1H, s) 8.81(1H, d) 7.58(1h, d) 7.24–7.45(5H)5.99(2H, d) 3.98(2H, s) 2.28(1H, s) A-740 11.34(1H) 9.12(1H, s) 8.78(1H,d) 7.56(1H, d) 7.25–7.40(5H) 4.60–4.67(3H) 3.43–3.66(4H) 3.41(2H, d)1.16(6H, t) A-1321 9.11(1H, s) 8.78(1H, d) 7.59(1H, d) 7.44–7.50(3H)7.29(2H, d) 3.53(3H, s) 2.44(3H, s) A-1322 9.10(1H, s) 8.78(1H, d)7.59(1H, d) 7.45–7.50(3H) 7.33(2H, d) 3.51(3H, s) 3.01(2H, q) 1.24(3H,t) A-776 9.17(1H, s) 8.76(1H, d) 7.57(1H, d) 7.25–7.40(5H) 5.89(1H, m)5.25(1H, d) 5.18(1H, d) 4.87(2H, s) 3.78(2H, d) 3.16(3H, s) A-10639.11(1H, s) 8.75(1H, d) 7.55(1H, d) 3.65(4H, dt) 2.56(3H, s) 2.05(4H, m)A-1108 9.14(1H, s) 8.76(1H, d) 7.57(1H, d) 5.86(1H, m) 5.24(1H, d)5.17(1H, d) 3.70–3.77(3H) 1.67–1.83(6H) A-1145 9.15(1H, s) 8.79(1H, d)7.58(1H, d) 5.84(1H, m) 5.26(1H, d) 5.19(1H, d) 3.81(8H) 3.72(2H, d)A-1275 9.26(1H, s) 8.83(1H, d)7.62(1H, d)7.38(2H, d) 7.27(2H, d)5.85(1H, m) 5.23(1h, d) 5.14(1H, d) 3.81(2H, d) A-1279 9.23(1H, s)8.83(1H, d) 7.61(1H, d) 7.15–7.40(9H) 4.40(2H, s) A-1324 9.11(1H, s)8.77(1H, d) 7.59(1H, d) 7.43–7.50(3H) 7.33(2H) 3.77(1H, m) 3.49(3H, s)1.30(6H, d) A-1325 9.15(1H, s) 8.78(1H, d) 7.60(1H, d) 7.35–7.50(3H)7.30(2H) 5.78(1H, m) 5.18(1H, d) 5.11(1H, d) 3.65(2H, d) 3.51(3H, s)A-1329 9.17(1H, s) 8.80(1H, d) 7.60(1H, d) 7.25–7.53(5H) 3.76(2H, s)3.65(3H, s) 3.48(3H, s) A-1332 9.11(1H, s) 8.78(1H, d) 7.59(1H, d)7.20–7.48(10H) 4.25(2H, s) 3.52(3H, s) A-1432 8.95(1H, s) 8.74(1H, d)7.54(1H, d) 7.25–7.43(5H) 5.86(1H, m) 5.21(1H, d) 5.14(1H, d) 3.69(2H,d) 2.09(3H, s) 1.95(3H, s) A-1437 9.29(1H, s) 8.85(1H, d) 7.50–7.68(5H)5.90(1H, m) 5.24(1H, d) 5.09(1H, d) 3.84(2H, d) A-1438 12.64(1H)9.24(1H, s) 8.85(1H, d) 7.15–7.70(9H) 4.43(2H, s) C-43 9.17(1H, s)8.84(1H, d) 7.60(1H, d) 5.89(1H, m) 5.28(1H, d) 5.19(1H, d) 4.54(2H, q)3.63(2H, d) 1.41(3H, t) C-612 11.37(1H) 9.18(1H, s) 8.79(1H, d) 7.57(1H,d) 7.28–7.40(5H) 5.91(1H, m) 5.25(1H, d) 5.14(1H, d) 4.60(2H, d)3.87(2H, d) D-1 9.75(1H) 9.17(1H, s) 8.82(1H, d) 7.59(1H, d) 3.45(2H, t)3.27(2H, t) D-2 9.20(1H, s) 8.80(1H, d) 7.57(1H, d) 3.75(2H, t) 3.25(2H,t) 3.23(3H, s) D-3 9.19(1H, s) 8.79(1H, d) 7.57(1H, d) 3.71–3.80(4H)3.23(2H, t) 1.23(3H, t) D-5 9.18(1H, s) 8.79(1H, d) 7.57(1H, d) 4.97(1H,m) 3.79(2H, t) 3.19(2H, t) 1.28(6H, d) D-9 9.16(1H, s) 8.80(1H, d)7.58(1H, d) 3.85(2H, t) 3.09(1H, t) 1.58(8H, s) D-40 9.21(1H, s)8.79(1H, d) 7.58(1H, d) 7.23–7.40(5H) 4.90(2H, s) 3.63(2H, t) 3.19(2H,t) D-60 9.09(1H, s) 8.75(1H, d) 7.53(1H, d) 7.41–7.44(4H) 7.30(1H)4.18(1H, t) 3.36(1H, t) D-63 9.07(1H, s) 8.77(1H, d) 7.55(1H, d)7.30–7.45(4H) 4.15(2H, t) 3.37(2H, t) D-104 9.31(1H, s) 8.91(1H, d)7.66(1H, d) 3.90(2H, s) 3.38(3H, s) D-107 9.29(1H, s) 8.90(1H, d)7.66(1H, d) 5.02(1H, m) 3.77(2H, s) 1.51(6H, d) D-111 9.23(1H, s)8.90(1H, d) 7.66(1H, d) 3.75(2H, s) 1.78(9H, s) D-143 9.25(1H, s)8.91(1H, d) 7.66(1H, d) 7.25–7.42(5H) 5.09(2H, s) 3.88(2H, s) D-1669.04(1H, s) 8.84(1H, d) 7.59(1H, d) 7.50(2H, d) 7.24(2H, d) 4.05(2H, s)D-207 9.31(1H, s) 8.90(1H, d) 4.06(1H, q) 3.38(3H, s) 1.71(3H, d) D-2109.29(1H, s) 8.90(1H, d) 7.66(1H, s) 5.02(1H, m) 4.10(1H, q) 1.68(3H, d)1.53(6H, d) D-246 9.23(1H, s) 8.89(1H, d) 7.65(1H, d) 7.25–7.38(5H)5.08(2H) 4.05(1H, q) 1.70(3H, d) D-269 9.04(1H, s) 8.83(1H, d) 7.58(1H,d) 7.47(2H, d) 7.24(2H, d) 4.21(1H, q) 1.80(3H, d) D-310 9.32(1H, s)8.90(1H, d) 7.66(1H, d) 3.39(3H, s) 1.69(6H, s) D-313 9.28(1H, s)8.88(1H, d) 7.65(1H, d) 5.00(1H, m) 1.63(6H, s) 1.50(6H, d) D-3499.20(1H, s) 9.87(1H, d) 7.64(1H, d) 7.20–7.40(5H) 5.10(2H, s) 1.68(6H,s) D-372 9.06(1H, s) 8.83(1H, d) 7.59(1H, d) 7.48(2H, d) 7.26(2H, d)1.80(6H, s) D-722 9.23(1H, s) 8.80(1H, d) 7.58(1H, d) 5.29(1H, d)3.84(1H, dd) 3.76(2H) 3.46(1H) 3.29(3H, s) 1.23(3H, t) D-825 9.45(1H)9.16(1H, s) 8.82(1H, d) 7.55(1H, d) 4.61(2H, t) 3.95(2H, t) E-1 9.30(1H,s) 8.84(1H, d) 8.43(1H, s) 7.64(1H, d) 4.09(3H, s) E-11 9.30(1H, s)8.86(1H, d) 8.47(1H, s) 7.64(1H, d) 6.02(1H, m) 5.32–3.36(2H) 5.08(1H,d) E-29 9.26(1H, s) 8.95(1H, s) 8.93(1H, d) 7.78(1H, d) 5.33(2H, s) (inacetone-d6) E-30 9.32(1H, s) 8.92(1H, d) 8.51(1H, s) 7.75(1H, d)5.24(2H, s) 3.82(3H, s) E-31 9.26(1H, s) 8.86(1H, d) 8.49(1H, s)7.63(1H, d) 5.21(2H, s) 4.27(2H, q) 1.29(3H, t) E-39 9.48(1H, s)9.10(1H, d) 8.58(1H, s) 8.24(1H, d) 7.27–7.43(5H) 5.66(2H, s) E-749.52(1H, s) 8.95(1H, d) 8.18(1H, d) 7.17(1H, d) 6.93(1H, d) 3.89(3H, s)E-102 9.21(1H, s) 8.87(1H, d) 7.73(1H, d) 7.58(1H, d) 7.09(1H, d)5.17(2H, s) (in acetone-d6) E-103 9.25(1H, s) 8.83(1H, d) 7.63(1H, d)7.10(1H, d) 6.83(1H, d) 5.01(2H, s) 3.81(3H, s) E-104 9.24(1H, s)8.82(1H, d) 7.61(1H, d) 7.09(1H, d) 6.82(1H, d) 4.98(2H, s) 4.26(2H, q)1.29(3H, t) E-112 9.45(1H, s) 9.03(1H, d) 8.23(1H, d) 7.37–7.45(3H)7.27(2H, d) 7.14(1H, d) 6.92(1H, d) 5.48(2H, s) E-537 9.27(1H, s)8.91(1H, d) 8.27(1H, s) 8.18(1H, d) 7.64–7.77(3H) F-12 9.34(1H, s)8.86(1H, d) 7.75(1H, d) 7.64(1H, d) 7.26–7.53(3H) 6.00(1H, m)5.12–5.32(2H) 5.13(1H, d) F-39 9.30(1H, s) 8.83(1H, d) 7.74(1H, d)7.62(1H, d) 7.24–7.43(8H) 5.73(2H, s) H-1 11.85(1H) 9.08(1H, s) 8.76(1H,d) 7.54(1H, d) 3.58(2H, m) 3.14(2H, m) 2.24(2H, m) G-1 9.18(1H, s)8.81(1H, d) 7.58(1H, d) 7.18–7.28(3H) 7.01(1H, d) 4.05(2H, s) K-18.90(1H, d) 8.77(1H, s) 7.63(1H, d) 4.36(2H, t) 3.65(2H, t)

According to a further feature of the present invention there isprovided a method for the control of pests at a locus which comprisesthe application of an effective amount of a compound of formula (I) or asalt thereof. For this purpose, the said compound is normally used inthe form of a pesticidal composition (i.e. in association withcompatible diluents or carriers and/or surface active agents suitablefor use in pesticidal compositions), for example as hereinafterdescribed.

The term “compound of the invention” as used hereinafter embraces a3-pyridylcarboxamide of formula (I) as defined above and a pesticidallyacceptable salt thereof.

One aspect of the present invention as defined above is a method for thecontrol of pests at a locus. The locus includes, for example, the pestitself, the place (plant, field, forest, orchard, waterway, soil, plantproduct, or the like) where the pest resides or feeds, or a placesusceptible to future infestation by the pest. The compound of theinvention may therefore be applied directly to the pest, to the placewhere the pest resides or feeds, or to the place susceptible to futureinfestation by the pest. As is evident from the foregoing pesticidaluses, the present invention provides pesticidally active compounds andmethods of use of said compounds for the control of a number of pestspecies which includes: arthropods, especially insects or mites, orplant nematodes. The compound of the invention may thus beadvantageously employed in practical uses, for example, in agriculturalor horticultural crops, in forestry, in veterinary medicine or livestockhusbandry, or in public health.

The compounds of the invention may be used for example in the followingapplications and on the following pests:

For the control of soil insects, such as corn rootworm, termites(especially for protection of structures), root maggots, wireworms, rootweevils, stalkborers, cutworms, root aphids, or grubs. They may also beused to provide activity against plant pathogenic nematodes, such asroot-knot, cyst, dagger, lesion, or stem or bulb nematodes, or againstmites. For the control of soil pests, for example corn rootworm, thecompounds are advantageously applied to or incorporated at an effectiverate into the soil in which crops are planted or to be planted or to theseeds or growing plant roots.

In the area of public health, the compounds are especially useful in thecontrol of many insects, especially filth flies or other Dipteran pests,such as houseflies, stableflies, soldierflies, hornflies, deerflies,horseflies, midges, punkies, blackflies, or mosquitoes.

In the protection of stored products, for example cereals, includinggrain or flour, groundnuts, animal feedstuffs, timber or householdgoods, e.g. carpets and textiles, compounds of the invention are usefulagainst attack by arthropods, more especially beetles, includingweevils, moths or mites, for example Ephestia spp. (flour moths),Anthrenus spp. (carpet beetles), Tribolium spp. (flour beetles),Sitophilus spp. (grain weevils) or Acarus spp. (mites).

In the control of cockroaches, ants or termites or similar arthropodpests in infested domestic or industrial premises or in the control ofmosquito larvae in waterways, wells, reservoirs or other running orstanding water.

For the treatment of foundations, structures or soil in the preventionof the attack on building by termites, for example, Reticuitermes spp.,Heterotermes spp., Coptotermes spp.

In agriculture against adults, larvae and eggs ofLepidoptera(butterflies and moths), e.g. Heliothis spp. such asHeliothis virescens (tobacco budworm), Heliothis armigera and Heliothiszea. Against adults and larvae of Coleoptera (beetles) e.g. Anthonomusspp. e.g. grandis (cotton boll weevil), Leptinotarsa decemlineata(Colorado potato beetle), Diabrotica spp. (corn rootworms). AgainstHeteroptera (Hemiptera and Homoptera) e.g. Psylla spp., Bemisia spp.,Trialeurodes spp., Aphis spp., Myzus spp., Megoura viciae, Phylloxeraspp., Nephotettix spp. (rice leaf hoppers), Nilaparvata spp.

Against Diptera e.g. Musca spp. Against Thysanoptera such as Thripstabaci.

Against Orthoptera such as Locusta and Schistocerca spp., (locusts andcrickets) e.g. Gryllus spp., and Acheta spp. for example, Blattaorientalis, Periplaneta americana, Blatella germanica, Locustamigratoria migratorioides, and Schistocerca gregaria. Against Collembolae.g. Periplaneta spp. and Blatella spp. (roaches). Against arthropods ofagricultural significance such as Acari (mites) e.g, Acarus siro, Argasspp., Ornithodoros spp., Dermanyssus gallinae, Eriophyes ribis,Phyllocoptruta oleivora, Boophilus spp., Rhipicephalus spp., Amblyommaspp., Hyalomma spp., Ixodes spp., Psoroptes spp., Chorioptes spp.,Sarcoptes spp., Tarsonemus spp., Bryobia praetiosa, Panonychus spp.,Tetranychus spp., Eotetranychus spp., Oligonychus spp., Eutetranychusspp.

From the order of the Isopoda, for example, Oniscus aselus, Armadiumvulgare, Porcellio scaber.

Against nematodes which attack plants or trees of importance toagriculture, forestry or horticulture either directly or by spreadingbacterial, viral, mycoplasma or fungal diseases of the plants. Theplant-parasitic nematodes which can be controlled in accordance with theinvention include, for example, the root-parasitic soil-dwellingnematodes such as, for example, those of the genera Meloidogyne (rootknot nematodes, such as Meloidogyne incognita, Meloidogyne hapla andMeloidogyne javanica), Heterodera and Globodera (cyst-forming nematodes,such as Globodera rostochiensis, Globodera pallida, Heterodera trifolii)and of the genera Radopholus, such as Radopholus similis, Pratylenchussuch as Pratylenchus neglectus, Pratylenchus penetrans and Pratylenchuscurvitatus;

Tylenchulus such as Tylenchulus semipenetrans, Tylenchorhynchus, such asTylenchorhynchus dubius and Tylenchorhynchus claytoni, Rotylenchus suchas Rotylenchus robustus, Heliocotylenchus such as Haliocotylenchusmulticinctus, Belonoaimus such as Belonoaimus longicaudatus, Longidorussuch as Longidorus elongatus, Trichodorus such as Trichodorus primitivusand Xiphinema such as Xiphinema index.

Other nematode genera which can be controlled using the compoundsaccording to the invention are Ditylenchus (stem parasites, such asDitylenchus dipsaci and Ditylenchus destructor), Aphelenchoides (foliarnematodes, such as Aphelenchoides ritzemabosi) and Anguina (seednematodes, such as Anguina tritici).

In the field of veterinary medicine or livestock husbandry or in themaintenance of public health against arthropods which are parasiticinternally or externally upon vertebrates, particularly warm-bloodedvertebrates, for example domestic animals, e.g. cattle, sheep, goats,equines, swine, poultry, dogs or cats, for example Acarina, includingticks (e.g. Ixodes spp, Boophilus spp. e.g. Boophilus microplus,Rhipicephalus spp. e.g. Rhipicephalus appendiculatus Ornithodorus spp.(e.g. Ornithodorus moubata) and mites (e.g. Damalinia spp.); fleas;Diptera (e.g. Aedes spp., Anopheles spp., Musca spp., Hypoderma spp.);Hemiptera; Dictyoptera (e.g. Periplaneta spp., Blatella spp.);Hymenoptera; for example against infections of the gastro-intestinaltract caused by parasitic nematode worms, for example members of thefamily Trichostrongylidae.

From the class of the helminths, for example, Haemonchus,Trichostrongulus, Ostertagia, Cooperia, Chabertia, Strongyloides,Oesophagostomum, Hyostrongulus, Ancylostoma, Ascaris and Heterakis andalso Fasciola.

From the class of the Gastropoda, for example, Deroceras spp., Arionspp., Lymnaea spp., Galba spp., Succinea spp., Biomphalaria spp.,Bulinus spp., Oncomelania spp.

From the class of the Bivalva, for example, Dreissena spp.

In practical use for the control of arthropods, especially insects oracarids, or nematode pests of plants, a method, for example, comprisesapplying to the plants or to the medium in which they grow an effectiveamount of a compound of the invention. For such a method, the compoundof the invention is generally applied to the locus in which thearthropod or nematode infestation is to be controlled at an effectiverate in the range of about 2 g to about 1 kg of the active compound perhectare of locus treated. Under ideal conditions, depending on the pestto be controlled, a lower rate may offer adequate protection. On theother hand, adverse weather conditions, resistance of the pest or otherfactors may require that the active ingredient be used at higher rates.The optimum rate depends usually upon a number of factors, for example,the type of pest being controlled, the type or the growth stage of theinfested plant, the row spacing or also the method of application.Preferably an effective rate range of the active compound is from about10 g/ha to about 400 g/ha, more preferably from about 50 g/ha to about200 g/ha.

When a pest is soil-borne, the active compound generally in a formulatedcomposition, is distributed evenly over the area to be treated (ie, forexample broadcast or band treatment) in any convenient manner and isapplied at rates from about 10 g/ha to about 400 g ai/ha, preferablyfrom about 50 g/ha to about 200 g ai/ha. When applied as a root dip toseedlings or drip irrigation to plants the liquid solution or suspensioncontains from about 0.075 to about 1000 mg ai/l, preferably from about25 to about 200 mg ai/l. Application may be made, if desired, to thefield or crop-growing area generally or in close proximity to the seedor plant to be protected from attack. The compound of the invention canbe washed into the soil by spraying with water over the area or can beleft to the natural action of rainfall. During or after application, theformulated compound can, if desired, be distributed mechanically in thesoil, for example by ploughing, disking, or use of drag chains.Application can be prior to planting, at planting, after planting butbefore sprouting has taken place, or after sprouting.

The compound of the invention and methods of control of pests therewithare of particular value in the protection of field, forage, plantation,glasshouse, orchard or vineyard crops, of ornamentals, or of plantationor forest trees, for example: cereals (such as wheat or rice), cotton,vegetables (such as peppers), field crops (such as sugar beets, soybeansor oil seed rape), grassland or forage crops (such as maize or sorghum),orchards or groves (such as of stone or pit fruit or citrus), ornamentalplants, flowers or vegetables or shrubs under glass or in gardens orparks, or forest trees (both deciduous and evergreen) in forests,plantations or nurseries.

They are also valuable in the protection of timber (standing, felled,converted, stored or structural) from attack, for example, by sawfliesor beetles or termites. They have applications in the protection ofstored products such as grains, fruits, nuts, spices or tobacco, whetherwhole, milled or compounded into products, from moth, beetle, mite orgrain weevil attack. Also protected are stored animal products such asskins, hair, wool or feathers in natural or converted form (e.g. ascarpets or textiles) from moth or beetle attack as well as stored meat,fish or grains from beetle, mite or fly attack.

Additionally, the compound of the invention and methods of use thereofare of particular value in the control of arthropods or helminths whichare injurious to, or spread or act as vectors of diseases domesticanimals, for example those hereinbefore mentioned, and more especiallyin the control of ticks, mites, lice, fleas, midges, or biting, nuisanceor myiasis flies. The compounds of the invention are particularly usefulin controlling arthropods or helminths which are present inside domestichost animals or which feed in or on the skin or suck the blood of theanimal, for which purpose they may be administered orally, parenterally,percutaneously or topically.

The compositions hereinafter described for application to growing cropsor crop growing loci or as a seed dressing may, in general,alternatively be employed in the protection of stored products,household goods, property or areas of the general environment. Suitablemeans of applying the compounds of the invention include: to growingcrops as foliar sprays (for example as an in-furrow spray), dusts,granules, fogs or foams or also as suspensions of finely divided orencapsulated compositions as soil or root treatments by liquid drenches,dusts, granules, smokes or foams; to seeds of crops via application asseed dressings by liquid slurries or dusts;

-   to animals infested by or exposed to infestation by arthropods or    helminths, by parenteral, oral or topical application of    compositions in which the active ingredient exhibits an immediate    and/or prolonged action over a period of time against the arthropods    or helminths, for example by incorporation in feed or suitable    orally-ingestible pharmaceutical formulations, edible baits, salt    licks, dietary supplements, pour-on formulations, sprays, baths,    dips, showers, jets, dusts, greases, shampoos, creams, wax smears or    livestock self-treatment systems;-   to the environment in general or to specific locations where pests    may lurk, including stored products, timber, household goods, or    domestic or industrial premises, as sprays, fogs, dusts, smokes,    wax-smears, lacquers, granules or baits, or in tricklefeeds to    waterways, wells, reservoirs or other running or standing water.

The compounds of the formula (I) can also be employed for controllingharmful organisms in crops of known genetically engineered plants orgenetically engineered plants yet to be developed. As a rule, thetransgenic plants are distinguished by especially advantageousproperties, for example by resistances to particular crop protectionagents, resistances to plant diseases or pathogens of plant diseases,such as particular insects or microorganisms such as fungi, bacteria orviruses. Other particular properties concern, for example, the harvestedmaterial with regard to quantity, quality, storage properties,composition and specific constituents. Thus, transgenic plants are knownwhere the starch content is increased, or the starch quality is altered,or where the harvested material has a different fatty acid composition.

The use in economically important transgenic crops of useful plants andornamentals is preferred, for example of cereals such as wheat, barley,rye, oats, millet, rice, cassaya and maize or else crops of sugar beet,cotton, soya, oilseed rape, potatoes, tomatoes, peas and other types ofvegetables.

When used in transgenic crops, in particular those which haveresistances to insects, effects are frequently observed, in addition tothe effects against harmful organisms to be observed in other crops,which are specific for application in the transgenic crop in question,for example an altered or specifically widened spectrum of pests whichcan be controlled, or altered application rates which may be employedfor application.

The invention therefore also relates to the use of compounds of theformula (I) for controlling harmful organisms in transgenic crop plants.

According to a further feature of the present invention there isprovided a pesticidal composition comprising one or more compounds ofthe invention as defined above, in association with, and preferablyhomogeneously dispersed in one or more compatible pesticidallyacceptable diluents or carriers and/or surface active agents [i.e.diluents or carriers and/or surface active agents of the type generallyaccepted in the art as being suitable for use in pesticidal compositionsand which are compatible with compounds of the invention].

In practice, the compounds of the invention most frequently form partsof compositions. These compositions can be employed to controlarthropods, especially insects and acarids, or helminths such as plantnematodes. The compositions may be of any type known in the art suitablefor application to the desired pest in any premises or indoor or outdoorarea. These compositions contain at least one compound of the inventionas the active ingredient in combination or association with one or moreother compatible components which are for example, solid or liquidcarriers or diluents, adjuvants, surface-active-agents, or the likeappropriate for the intended use and which are agronomically ormedicinally acceptable. These compositions, which may be prepared by anymanner known in the art, likewise form a part of this invention.

The compounds of the invention, in their commercially availableformulations and in the use forms prepared from these formulations maybe present in mixtures with other active substances such asinsecticides, attractants, sterilants, acaricides, nematicides,fungicides, growth regulatory substances or herbicides.

The pesticides include, for example, phosphoric esters, carbamates,carboxylic esters, formamidines, tin compounds and materials produced bymicroorganisms.

Preferred components in mixtures are:

1. from the group of the phosphorus compounds

acephate, azamethiphos, azinphos-ethyl, azinphos-methyl, bromophos,bromophos-ethyl, cadusafos (F-67825), chlorethoxyphos, chlorfenvinphos,chlormephos, chlorpyrifos, chlorpyrifos-methyl, demeton,demeton-S-methyl, demeton-S-methyl sulfone, dialifos, diazinon,dichlorvos, dicrotophos, dimethoate, disulfoton, EPN, ethion,ethoprophos, etrimfos, famphur, fenamiphos, fenitriothion,fensulfothion, fenthion, flupyrazofos, fonofos, formothion, fosthiazate,heptenophos, isazophos, isothioate, isoxathion, malathion, methacrifos,methamidophos, methidathion, salithion, mevinphos, monocrotophos, naled,omethoate, oxydemeton-methyl, parathion, parathion-methyl, phenthoate,phorate, phosalone, phosfolan, phosphocarb (BAS-301), phosmet,phosphamidon, phoxim, pirimiphos, pirimiphos-ethyl, pirimiphos-methyl,profenofos, propaphos, proetamphos, prothiofos, pyraclofos,pyridapenthion, quinalphos, sulprofos, temephos, terbufos, tebupirimfos,tetrachlorvinphos, thiometon, triazophos, trichlorphon, vamidothion;

2. from the group of the carbamates alanycarb (OK-135), aldicarb,2-sec-butylphenyl methylcarbamate (BPMC), carbaryl, carbofuran,carbosulfan, cloethocarb, benfuracarb, ethiofencarb, furathiocarb,HCN-801, isoprocarb, methomyl,5-methyl-m-cumenylbutyryl(methyl)carbamate, oxamyl, pirimicarb,propoxur, thiodicarb, thiofanox,1-methylthio(ethylideneamino)-N-methyl-N-(morpholinothio)carbamate (UC51717), triazamate;

3. from the group of the carboxylic esters

acrinathrin, allethrin, alphametrin, 5-benzyl-3-furylmethyl(E)-(1R)-cis-2,2-dimethyl-3-(2-oxothiolan-3-ylidenemethyl)cyclopropanecarboxylate,beta-cyfluthrin, alpha-cypermethrin, beta-cypermethrin, bioallethrin,bioallethrin ((S)-cyclopentylisomer), bioresmethrin, bifenthrin,(RS)-1-cyano-1-(6-phenoxy-2-pyridyl)methyl(1RS)-trans-3-(4-tert-butylphenyl)-2,2-dimethylcyclopropanecarboxylate(NCI 85193), cycloprothrin, cyfluthrin, cyhalothrin, cythithrin,cypermethrin, cyphenothrin, deltamethrin, empenthrin, esfenvalerate,fenfluthrin, fenpropathrin, fenvalerate, flucythrinate, flumethrin,fluvalinate (D isomer), imiprothrin (S-41311), lambda-cyhalothrin,permethrin, phenothrin (® isomer), prallethrin, pyrethrins (naturalproducts), resmethrin, tefluthrin, tetramethrin, theta-cypermethrin,tralomethrin, transfluthrin, zeta-cypermethrin (F-56701);

4. from the group of the amidines

amitraz, chlordimeform;

5. from the group of the tin compounds

cyhexatin, fenbutatin oxide;

6. others

abamectin, ABG-9008, acetamiprid, acequinocyl, Anagrapha falcitera,AKD-1022, AKD-3059, ANS-118, azadirachtin, Bacillus thuringiensis,Beauveria bassianea, bensultap, bifenazate, binapacryl, BJL-932,bromopropylate, BTG-504, BTG-505, buprofezin, camphechlor, cartap,chlorobenzilate, chlorfenapyr, chlorfluazuron,2-(4-chlorophenyl)-4,5-diphenylthiophene (UBI-T 930), chlorfentezine,chlorproxyfen, chromafenozide, clothianidine, 2-naphthylmethylcyclopropanecarboxylate (Ro12-0470), cyromazin, diacloden(thiamethoxam), diafenthiuron, DBI-3204, ethyl2-chloro-N-(3,5-dichloro-4-(1,1,2,3,3,3-hexafluoro-1-propyloxy)phenyl)carbamoyl)-2-carboximidate,DDT, dicofol, diflubenzuron,N-(2,3-dihydro-3-methyl-1,3-thiazol-2-ylidene)-2,4-xylidine,dihydroxymethyldihydroxypyrrolidine, dinobuton, dinocap, diofenolan,emamectin benzoate, endosulfan, ethiprole (sulfethiprole), ethofenprox,etoxazole, fenazaquin, fenoxycarb, fipronil, fluazuron, flumite(flufenzine, SZI-121),2-fluoro-5-(4-(4-ethoxyphenyl)₄-methyl-1-pentyl)diphenyl ether (MTI800), granulosis and nuclear polyhedrosis viruses, fenpyroximate,fenthiocarb, fluacrypyrim, flubenzimine, flubrocythrinate,flucycloxuron, flufenoxuron, flufenzine, flufenprox, fluproxyfen,gamma-HCH, halfenozide, halofenprox, hexaflumuron (DE_(—)473),hexythiazox, HOI-9004, hydramethylnon (AC 217300), IKI-220, indoxacarb,ivermectin, L-14165, imidacloprid, indoxacarb (DPX-MP062), kanemite(AKD-2023), lufenuron, M-020, M-020, methoxyfenozide, milbemectin,NC-196, neemgard, nidinoterfuran, nitenpyram,2-nitromethyl-4,5-dihydro-6H-thiazine (DS 52618),2-nitromethyl-3,4-dihydrothiazole (SD 35651),2-nitromethylene-1,2-thiazinan-3-ylcarbamaldehyde (WL 108477),novaluron, pirydaryl, propargite, protrifenbute, pymethrozine,pyridaben, pyrimidifen, pyriproxyfen, NC-196, NC-1111, NNI-9768,novaluron (MCW-275), OK-9701, OK-9601, OK-9602, OK-9802, R-195, RH-0345,RH-2485, RYI-210, S-1283, S-1-833, SI-8601, silafluofen, silomadine(CG-177), spinosad, spirodiclofen, SU-9118, tebufenozide, tebufenpyrad,teflubenzuron, tetradifon, tetrasul, thiacloprid, thiocyclam,thiamethoxam, tolfenpyrad, triazamate, triethoxyspinosyn A, triflumuron,verbutin, vertalec (mykotal), YI-5301.

The abovementioned components for combinations are known activesubstances, many of which are described in Ch. R Worthing, S. B. Walker,The Pesticide Manual, 12^(th) Edition, British Crop Protection Council,Farnham 2000.

The effective use doses of the compounds employed in the invention canvary within wide limits, particularly depending on the nature of thepest to be eliminated or degree of infestation, for example, of cropswith these pests. In general, the compositions according to theinvention usually contain about 0.05 to about 95% (by weight) of one ormore active ingredients according to the invention, about 1 to about 95%of one or more solid or liquid carriers and, optionally, about 0.1 toabout 50% of one or more other compatible components, such assurface-active agents or the like. In the present account, the term“carrier” denotes an organic or inorganic ingredient, natural orsynthetic, with which the active ingredient is combined to facilitateits application, for example, to the plant, to seeds or to the soil.This carrier is therefore generally inert and it must be acceptable (forexample, agronomically acceptable, particularly to the treated plant).

The carrier may be a solid, for example, clays, natural or syntheticsilicates, silica, resins, waxes, solid fertilizers (for exampleammonium salts), ground natural minerals, such as kaolins, clays, talc,chalk, quartz, attapulgite, montmorillonite, bentonite or diatomaceousearth, or ground synthetic minerals, such as silica, alumina, orsilicates especially aluminium or magnesium silicates. As solid carriersfor granules the following are suitable: crushed or fractionated naturalrocks such as calcite, marble, pumice, sepiolite and dolomite; syntheticgranules of inorganic or organic meals; granules of organic materialsuch as sawdust, coconut shells, corn cobs, corn husks or tobaccostalks; kieselguhr, tricalcium phosphate, powdered cork, or absorbentcarbon black; water soluble polymers, resins, waxes; or solidfertilizers. Such solid compositions may, if desired, contain one ormore compatible wetting, dispersing, emulsifying or colouring agentswhich, when solid, may also serve as a diluent.

The carrier may also be liquid, for example: water; alcohols,particularly butanol or glycol, as well as their ethers or esters,particularly methylglycol acetate; ketones, particularly acetone,cyclohexanone, methylethyl ketone, methylisobutylketone, or isophorone;petroleum fractions such as paraffinic or aromatic hydrocarbons,particularly xylenes or alkyl naphthalenes; mineral or vegetable oils;aliphatic chlorinated hydrocarbons, particularly trichloroethane ormethylene chloride; aromatic chlorinated hydrocarbons, particularlychlorobenzenes; water-soluble or strongly polar solvents such asdimethylformamide, dimethyl sulphoxide, or N-methylpyrrolidone;liquefied gases; or the like or a mixture thereof.

The surface-active agent may be an emulsifying agent, dispersing agentor wetting agent of the ionic or non-ionic type or a mixture of suchsurface-active agents. Amongst these are e.g., salts of polyacrylicacids, salts of lignosulphonic acids, salts of phenolsulphonic ornaphthalenesulphonic acids, polycondensates of ethylene oxide with fattyalcohols or fatty acids or fatty esters or fatty amines, substitutedphenols (particularly alkylphenols or arylphenols), salts ofsulphosuccinic acid esters, taurine derivatives (particularlyalkyltaurates), phosphoric esters of alcohols or of polycondensates ofethylene oxide with phenols, esters of fatty acids with polyols, orsulphate, sulphonate or phosphate functional derivatives of the abovecompounds. The presence of at least one surface-active agent isgenerally essential when the active ingredient and/or the inert carrierare only slightly water soluble or are not water soluble and the carrieragent of the composition for application is water. Compositions of theinvention may further contain other additives such as adhesives orcolorants. Adhesives such as carboxymethylcellulose or natural orsynthetic polymers in the form of powders, granules or lattices, such asarabic gum, polyvinyl alcohol or polyvinyl acetate, naturalphospholipids, such as cephalins or lecithins, or syntheticphospholipids can be used in the formulations. It is possible to usecolorants such as inorganic pigments, for example: iron oxides, titaniumoxides or Prussian Blue; organic dyestuffs, such as alizarin dyestuffs,azo dyestuffs or metal phthalocyanine dyestuffs; or trace nutrients suchas salts of iron, manganese, boron, copper, cobalt, molybdenum or zinc.

For their agricultural application, the compounds of the invention aretherefore generally in the form of compositions, which are in varioussolid or liquid forms. Solid forms of compositions which can be used aredusting powders (with a content of the compound of the invention,ranging up to 80%), wettable powders or granules (including waterdispersible granules), particularly those obtained by extrusion,compacting, impregnation of a granular carrier, or granulation startingfrom a powder (the content of the compound of the invention, in thesewettable powders or granules being between about 0.5 and about 80%).Solid homogenous or heterogenous compositions containing one or morecompounds of the invention, for example granules, pellets, briquettes orcapsules, may be used to treat standing or running water over a periodof time. A similar effect may be achieved using trickle or intermittentfeeds of water dispersible concentrates as described herein. Liquidcompositions, for example, include aqueous or non-aqueous solutions orsuspensions (such as emulsifiable concentrates, emulsions, flowables,dispersions, or solutions) or aerosols. Liquid compositions alsoinclude, in particular, emulsifiable concentrates, dispersions,emulsions, flowables, aerosols, wettable powders (or powder forspraying), dry flowables or pastes as forms of compositions which areliquid or intended to form liquid compositions when applied, for exampleas aqueous sprays (including low and ultra-low volume) or as fogs oraerosols.

Liquid compositions, for example, in the form of emulsifiable or solubleconcentrates most frequently comprise about 5 to about 80% by weight ofthe active ingredient, while the emulsions or solutions which are readyfor application contain, in their case, about 0.01 to about 20% of theactive ingredient. Besides the solvent, the emulsifiable or solubleconcentrates may contain, when required, about 2 to about 50% ofsuitable additives, such as stabilizers, surface-active agents,penetrating agents, corrosion inhibitors, colorants or adhesives.Emulsions of any required concentration, which are particularly suitablefor application, for example, to plants, may be obtained from theseconcentrates by dilution with water. These compositions are includedwithin the scope of the compositions which may be employed in thepresent invention. The emulsions may be in the form of water-in-oil oroil-in-water type and they may have a thick consistency.

The liquid compositions of this invention may, in addition to normalagricultural use applications be used for example to treat substrates orsites infested or liable to infestation by arthropods (or other pestscontrolled by compounds of this invention) including premises, outdooror indoor storage or processing areas, containers or equipment orstanding or running water.

All these aqueous dispersions or emulsions or spraying mixtures can beapplied, for example, to crops by any suitable means, chiefly byspraying, at rates which are generally of the order of about 100 toabout 1,200 liters of spraying mixture per hectare, but may be higher orlower (eg. low or ultra-low volume) depending upon the need orapplication technique. The compound or compositions according to theinvention are conveniently applied to vegetation and in particular toroots or leaves having pests to be eliminated. Another method ofapplication of the compounds or compositions according to the inventionis by chemigation, that is to say, the addition of a formulationcontaining the active ingredient to irrigation water. This irrigationmay be sprinkler irrigation for foliar pesticides or it can be groundirrigation or underground irrigation for soil or for systemicpesticides.

The concentrated suspensions, which can be applied by spraying, areprepared so as to produce a stable fluid product which does not settle(fine grinding) and usually contain from about 10 to about 75% by weightof active ingredient, from about 0.5 to about 30% of surface-activeagents, from about 0.1 to about 10% of thixotropic agents, from about 0to about 30% of suitable additives, such as anti-foaming agents,corrosion inhibitors, stabilizers, penetrating agents, adhesives and, asthe carrier, water or an organic liquid in which the active ingredientis poorly soluble or insoluble Some organic solids or inorganic saltsmay be dissolved in the carrier to help prevent settling or asantifreezes for water.

The wettable powers (or powder for spraying) are usually prepared sothat they contain from about 10 to about 80% by weight of activeingredient, from about 20 to about 90% of a solid carrier, from about 0to about 5% of a wetting agent, from about 3 to about 10% of adispersing agent and, when necessary, from about 0 to about 80% of oneor more stabilizers and/or other additives, such as penetrating agents,adhesives, anti-caking agents, colorants, or the like. To obtain thesewettable powders, the active ingredient is thoroughly mixed in asuitable blender with additional substances which may be impregnated onthe porous filler and is ground using a mill or other suitable grinder.This produces wettable powders, the wettability and the suspendabilityof which are advantageous. They may be suspended in water to give anydesired concentration and this suspension can be employed veryadvantageously in particular for application to plant foliage.

The “water dispersible granules (WG)” (granules which are readilydispersible in water) have compositions which are substantially close tothat of the wettable powders. They may be prepared by granulation offormulations described for the wettable powders, either by a wet route(contacting finely divided active ingredient with the inert filler and alittle water, e.g. 1 to 20% by weight, or with an aqueous solution of adispersing agent or binder, followed by drying and screening), or by adry route (compacting followed by grinding and screening).

The rates and concentrations of the formulated compositions may varyaccording to the method of application or the nature of the compositionsor use thereof. Generally speaking, the compositions for application tocontrol arthropod or helminth pests usually contain from about 0.00001%to about 95%, more particularly from about 0.0005% to about 50% byweight of one or more compounds of the invention, or of total activeingredients (that is to say the compounds of the invention, togetherwith other substances toxic to arthropods or helminths, synergists,trace elements or stabilizers). The actual compositions employed andtheir rate of application will be selected to achieve the desiredeffect(s) by the farmer, livestock producer, medical or veterinarypractitioner, pest control operator or other person skilled in the art.Solid or liquid compositions for application topically to animals,timber, stored products or household goods usually contain from about0.00005% to about 90%, more particularly from about 0.001% to about 10%,by weight of one or more compounds of the invention. For administrationto animals orally or parenterally, including percutaneously solid orliquid compositions, these normally contain from about 0.1% to about 90%by weight of one or more compounds of the invention. Medicatedfeedstuffs normally contain from about 0.001% to about 3% by weight ofone or more compounds of the invention. Concentrates or supplements formixing with feedstuffs normally contain from about 5% to about 90%,preferably from about 5% to about 50%, by weight of one or morecompounds of the invention. Mineral salt licks normally contain fromabout 0.1% to about 10% by weight of one or more compounds of formula(I) or pesticidally acceptable salts thereof.

Dusts or liquid compositions for application to livestock, goods,premises or outdoor areas may contain from about 0.0001% to about 15%,more especially from about 0.005% to about 2.0%, by weight, of one ormore compounds of the invention.

Suitable concentrations in treated waters are between about 0.0001 ppmand about 20 ppm, more particularly about 0.001 ppm to about 5.0 ppm. ofone or more compounds of the invention, and may be used therapeuticallyin fish farming with appropriate exposure times. Edible baits maycontain from about 0.01% to about 5%, preferably from about 0.01% toabout 1.0%, by weight, of one or more compounds of the invention.

When administered to vertebrates parenterally, orally or by percutaneousor other means, the dosage of compounds of the invention, will dependupon the species, age, or health of the vertebrate and upon the natureand degree of its actual or potential infestation by arthropod orhelminth pests. A single dose of about 0.1 to about 100 mg, preferablyabout 2.0 to about 20.0 mg, per kg body weight of the animal or doses ofabout 0.01 to about 20.0 mg, preferably about 0.1 to about 5.0 mg, perkg body weight of the animal per day, for sustained medication, aregenerally suitable by oral or parenteral administration. By use ofsustained release formulations or devices, the daily doses required overa period of months may be combined and administered to animals on asingle occasion.

The following composition EXAMPLES 2A-2M illustrate compositions for useagainst arthropods, especially insects or acarids, or helminths such asplant nematodes, which comprise, as active ingredient, compounds of theinvention, such as those described in preparative examples. Thecompositions described in EXAMPLES 2A-2M can each be diluted to give asprayable compositon at concentrations suitable for use in the field.Generic chemical descriptions of the ingredients (for which all of thefollowing percentages are in weight percent), used in the compositionEXAMPLES 2A-2M exemplified below, are as follows:

Trade Name Chemical Description Ethylan BCP Nonylphenol ethylene oxidecondensate Soprophor BSU Tristyrylphenol ethylene oxide condensateArylan CA A 70% w/v solution of calcium dodecylbenzenesulfonate Solvesso150 Light C₁₀ aromatic solvent Arylan S Sodium dodecylbenzenesulfonateDarvan NO₂ Sodium lignosulphonate Celite PF Synthetic magnesium silicatecarrier Sopropon T36 Sodium salts of polycarboxylic acids Rhodigel 23Polysaccharide xanthan gum Bentone 38 Organic derivative of magnesiummontmorillonite Aerosil Microfine silicon dioxide

Example 2A

A water soluble concentrate is prepared with the composition as follows:

Active ingredient  7% Ethylan BCP 10% N-methylpyrrolidone 83%

To a solution of Ethylan BCP dissolved in a portion ofN-methylpyrrolidone is added the active ingredient with heating andstirring until dissolved. The resulting solution is made up to volumewith the remainder of the solvent.

Example 2B

An emulsifiable concentrate (EC) is prepared with the composition asfollows:

Active ingredient 25% (max) Soprophor BSU 10% Arylan CA  5%N-methylpyrrolidone 50% Solvesso 150 10%

The first three components are dissolved in N-methylpyrrolidone and tothis is then added the Solvesso 150 to give the final volume.

Example 2C

A wettable powder (WP) is prepared with the composition as follows:

Active ingredient 40% Arylan S  2% Darvan NO₂  5% Celite PF 53%

The ingredients are mixed and ground in a hammer-mill to a powder with aparticle size of less than 50 microns.

Example 2D

An aqueous-flowable formulation is prepared with the composition asfollows:

Active ingredient 40.00% Ethylan BCP 1.00% Sopropon T360. 0.20% Ethyleneglycol 5.00% Rhodigel 230. 0.15% Water 53.65%

The ingredients are intimately mixed and are ground in a bead mill untila mean particle size of less than 3 microns is obtained.

Example 2E

An emulsifiable suspension concentrate is prepared with the compositionas follows:

Active ingredient 30.0% Ethylan BCP 10.0% Bentone 38 0.5% Solvesso 15059.5%

The ingredients are intimately mixed and ground in a beadmill until amean particle size of less than 3 microns is obtained.

Example 2F

A water dispersible granule is prepared with the composition as follows:

Active ingredient 30% Darvan No 2 15% Arylan S  8% Celite PF 47%

The ingredients are mixed, micronized in a fluid-energy mill and thengranulated in a rotating pelletizer by spraying with water (up to 10%).The resulting granules are dried in a fluid-bed drier to remove excesswater.

Example 2G

A dusting powder is prepared with the composition as follows:

Active ingredient  1 to 10% Talc powder-superfine 99 to 90%

The ingredients are intimately mixed and further ground as necessary toachieve a fine powder. This powder may be applied to a locus ofarthropod infestation, for example refuse dumps, stored products orhousehold goods or animals infested by, or at risk of infestation by,arthropods to control the arthropods by oral ingestion. Suitable meansfor distributing the dusting powder to the locus of arthropodinfestation include mechanical blowers, handshakers or livestock selftreatment devices.

Example 2H

An edible bait is prepared with the composition as follows:

Active ingredient 0.1 to 1.0% Wheat flour 80% Molasses 19.9 to 19%  

The ingredients are intimately mixed and formed as required into a baitform. This edible bait may be distributed at a locus, for exampledomestic or industrial premises, e.g. kitchens, hospitals or stores, oroutdoor areas, infested by arthropods, for example ants, locusts,cockroaches or flies, to control the arthropods by oral ingestion.

Example 2I

A solution formulation is prepared with a composition as follows:

Active ingredient 15% Dimethyl sulfoxide 85%

The active ingredient is dissolved in dimethyl sulfoxide with mixing andor heating as required. This solution may be applied percutaneously as apour-on application to domestic animals infested by arthropods or, aftersterilization by filtration through a polytetrafluoroethylene membrane(0.22 micrometer pore size), by parenteral injection, at a rate ofapplication of from 1.2 to 12 ml of solution per 100 kg of animal bodyweight.

Example 2J

A wettable powder is prepared with the composition as follows:

Active ingredient 50% Ethylan BCP 5% Aerosil 5% Celite PF 40%

The Ethylan BCP is absorbed onto the Aerosil which is then mixed withthe other ingredients and ground in a hammer-mill to give a wettablepowder, which may be diluted with water to a concentration of from0.001% to 2% by weight of the active compound and applied to a locus ofinfestation by arthropods, for example, dipterous larvae or plantnematodes, by spraying, or to domestic animals infested by, or at riskof infection by arthropods, by spraying or dipping, or by oraladministration in drinking water, to control the arthropods.

Example 2K

A slow release bolus composition is formed from granules containing thefollowing components in varying percentages (similar to those describedfor the previous compositions) depending upon need:

-   -   Active ingredient    -   Density agent    -   Slow-release agent    -   Binder

The intimately mixed ingredients are formed into granules which arecompressed into a bolus with a specific gravity of 2 or more. This canbe administered orally to ruminant domestic animals for retention withinthe reticulo-rumen to give a continual slow release of active compoundover an extended period of time to control infestation of the ruminantdomestic animals by arthropods.

Example 2L

A slow release composition in the form of granules, pellets, brickettesor the like can be prepared with compositions as follows:

Active ingredient 0.5 to 25% Polyvinyl chloride  75 to 99.5% Dioctylphthalate (plasticizer)

The components are blended and then formed into suitable shapes bymelt-extrusion or molding. These composition are useful, for example,for addition to standing water or for fabrication into collars oreartags for attachment to domestic animals to control pests by slowrelease.

Example 2M

A water dispersible granule is prepared with the composition as follows:

Active ingredient 85% (max) Polyvinylpyrrolidone  5% Attapulgite clay 6% Sodium lauryl sulfate  2% Glycerine  2%

The ingredients are mixed as a 45% slurry with water and wet milled to aparticle size of 4 microns, then spray-dried to remove water.

Methods of Pesticidal Use

The following representative test procedures, using compounds of theinvention, were conducted to determine the parasiticidal and pesticidalactivity of compounds of the invention.

Method A:

Germinated field bean seeds (Vicia faba) with seed roots weretransferred into brown glass bottles filled with tap water and thenpopulated with about 100 black bean aphids (Aphis fabae). Plants andaphids were then dipped into an aqueous solution of the formulatedpreparation to be examined for 5 seconds. After they had drained, plantsand animals were stored in a climatized chamber (16 hours of light/day,25° C., 40-60% relative atmospheric humidity). After 3 and 6 days ofstorage, the effect of the preparation on the aphids was determined. Ata concentration of 100 ppm (based on the content of active compound),the following Compounds caused a mortality of at least 50% among theaphids:

-   A-53, A-59, A-67, A-72, A-94, A-95, A-102, A-229, A-230, A-237,    A-437, A-438, A-439, A-458, A-460, A-489, A-576, A-714, A-715,    A-724, A-733, A-776, A-1063, A-1108, A-1145, A-1275, A-1279, A-1321,    A-1322, A-1324, A-1325, A-1329, A-1432, A-1437, A-1438, C-43, D-2,    D-3, D-5, D-8, D-104, D-111, D-143, D-210, D-246, D-269, D-313,    D-349, E-74, G-1, H-1 and K-1.    Method B:

Germinated field bean seeds (Vicia faba) with seed roots weretransferred into brown glass bottles filled with tap water. Fourmilliliters of an aqueous solution of the formulated preparation to beexamined were pipetted into the brown glass bottle.

The field bean was then heavily populated with about 100 black beanaphids (Aphis fabae). Plants and aphids were then stored in a climatizedchamber (16 hours of light/day, 25° C., 40-60% relative atmospherichumidity). After 3 and 6 days of storage, the root-systemic effect ofthe preparation on the aphids was determined. At a concentration of 10ppm (based on the content of active compound), The following Compoundscaused a mortality of at least 80% among the aphids, by root-systemicaction:

-   A-53, A-54, A-56, A-59, A-67, A-72, A-84, A-89, A-94, A-95, A-102,    A-438, A-576, A-714, A-715, A-724, A-733, A-740, A-776, A-1063,    A-1108, A-1145, A-1275, A-1321, A-1322, A-1324, A-1325, A-1329,    A-1332, C-43, D-2, D-3, D-5, D-104, D-111, D-210, D-269, D-313,    D-372, E-1, E-74, G-1, H-1 and K-1.

1. A compound of the formula (I):

wherein: N=Q is a formula (A) or (B):

Z is YR¹; or when Z is YR¹, R¹ and R³ may form together with theadjacent —Y—C—NR²— atoms, a five or six membered saturated heterocyclicring which optionally contains an additional N or O atom, and isunsubstituted or substituted by one or more R⁷ groups or one of the ringcarbon atoms may form a carbonyl or imino group, and which ring isoptionally fused to a benzene ring optionally substituted by R⁷; or whenZ is YR¹, R¹ and R³ may form together with the adjacent —Y—C—NR²— atoms,a group (A²):

Y, X and W are each independently O or S; or R¹ and R⁴ may form togetherwith the adjacent —X—C—W— group, a five or six membered unsaturated,partially saturated or saturated heterocyclic ring, unsubstituted orsubstituted by one or more R⁷ groups or one of the ring carbon atoms mayform a carbonyl group; R¹ is (C₁-C₈)alkyl, (C₃-C₆)alkenyl,(C₃-C₆)alkynyl or (C₃-C₈)cycloalkyl, which last four mentioned groupsare unsubstituted or substituted by one or more R⁸ groups; or is(C₃-C₈)cycloalkyl-(C₁-C₆)alkyl which cycloalkyl is unsubstituted orsubstituted by one or more R⁸ groups; or is —(CR⁹R¹⁰)_(p)R¹¹ or—(CR⁹R¹⁰)_(p)heterocyclyl; or when Y is O is (C₁-C₆)alkylamino,NH(C₃-C₈)cycloalkyl or NH(CH₂)_(n)R¹¹; R^(2a) is (C₁-C₈)alkyl,(C₃-C₆)alkenyl, (C₃-C₆)alkynyl, (C₃-C₈)cycloalkyl, (C₁-C₆)alkoxy,(C₃-C₆)alkenyloxy, (C₃-C₆)alkynyloxy, (C₁-C₆)alkylamino,di-(C₁-C₆)alkylamino, NHCO(C₁-C₆)alkyl, NHSO₂(C₁-C₆)alkyl,CO(C₁-C₆)alkyl or SO₂(C₁-C₆)alkyl which last thirteen mentioned groupsare unsubstituted or substituted by one or more R⁸ groups; or is(C₃-C₈)cycloalkyl-(C₁-C₆)alkyl which cycloalkyl is unsubstituted orsubstituted by one or more R⁸ groups; or is —(CR⁹R¹⁰)_(p)R¹¹,—(CR⁹R¹⁰)_(p)heterocyclyl, OH, SO₂R¹¹, NH₂, NHCOR¹¹, NHR¹¹,NH(C₃-C₈)cycloalkyl, NH(CH₂)_(s)R¹¹, O(CHR¹⁰)_(r)R¹¹;O(CH₂)_(r)heterocyclyl or N═C[(C₁-C₆)alkyl]₂; or is (C₃-C₆)alkenylsubstituted by R¹¹; R² is R^(2a) or H; R³ is H or R¹; R⁴ is (C₁-C₆)alkylsubstituted by R⁸; or is (C₃-C₆)alkenyl, (C₃-C₆)alkynyl or(C₃-C₈)cycloalkyl which last three mentioned groups are unsubstituted orsubstituted by one or more R⁸ groups; or is(C₃-C₈)cycloalkyl-(C₁-C₆)alkyl unsubstituted or substituted by one ormore R⁸ groups; or is —(CR⁹R¹⁰)_(p)R¹¹ or —(CR⁹R¹⁰)_(p)heterocyclyl; orwhen W is O, R⁴ is (C₁-C₆)alkylamino; or R² and R³ together with theadjacent N atom form a 3 to 8-membered unsaturated, partially saturatedor saturated heterocyclic ring which optionally contains up to threeadditional N, O or S atoms and which ring is unsubstituted orsubstituted by one or more R⁷ groups; R⁷ is R⁸, R⁴, (C₁-C₆)alkyl orCH₂OH; R⁸ is halogen, (C₁-C₆)alkoxy, (C₁-C₆)haloalkoxy, S(O)_(n)R¹², CN,CO₂(C₁-C₆)alkyl, CO₂H, NO₂, OH, amino, (C₁-C₆)alkylamino,di-(C₁-C₆)alkylamino, carbamoyl, (C₁-C₆)-alkylcarbamoyl,di-(C₁-C₆)-alkylcarbamoyl, CH[O(C₁-C₆)alkyl]₂, (C₃-C₆)alkenyloxy,(C₃-C₆)alkynyloxy or O(CH₂)_(r)R¹¹; R⁹ and R¹⁰ are each independently H,(C₁-C₆)alkyl or (C₁-C₆)haloalkyl; R¹¹ is aryl unsubstituted orsubstituted by one or more groups selected from (C₁-C₆)alkyl,(C₁-C₆)haloalkyl, (C₂-C₆)alkenyl, (C₂-C₆)alkynyl, (C₃-C₈)cycloalkyl,—(CH₂)_(u)R¹³, heterocyclyl, halogen, (C₁-C₆)alkoxy, (C₁-C₆)haloalkoxy,S(O)_(n)R¹², CN, CO₂(C₁-C₆)alkyl, NO₂, amino, (C₁-C₆)alkylamino anddi-(C₁-C₆)alkylamino; R¹² is (C₁-C₆)alkyl or (C₁-C₆)haloalkyl; R¹³ isphenyl unsubstituted or substituted by one or more groups selected fromhalogen, (C₁-C₆)alkyl and (C₁-C₆)haloalkyl; R^(e) is H, (C₁-C₆)alkyl,(C₂-C₆)alkenyl, (C₂-C₆)alkynyl, (C₃-C₈)cycloalkyl,(C₃-C₈)cycloalkyl-(C₁-C₆)alkyl, halogen, (C₁-C₆)alkoxy,(C₁-C₆)haloalkoxy, S(O)_(n)R², (C₃-C₆)alkenyloxy, (C₃-C₆)alkynyloxy,—(CH₂)_(p)R¹¹, heterocyclyl, CN, CO₂(C₁-C₆)alkyl, NO₂, amino,(C₁-C₆)alkylamino, di-(C₁-C₆)alkylamino or O(CH₂)_(r)R¹¹ wherein r is 0or 1; U is N or CH, m, s and u are each independently 0 or 1; n is 0, 1or 2; p is 0, 1, 2 or 3; r is 0 or an integer from 1 to 6; and eachheterocyclyl in the above mentioned radicals is independently a mono orbicyclic heterocyclic radical having 3 to 7 ring atoms in each ring and1 to 4 hetero atoms selected from N, O and S; or a pesticidallyacceptable salt thereof.
 2. A compound or a salt thereof as claimed inclaim 1, wherein R¹ is (C₁-C₈)alkyl or (C₃-C₆)alkenyl, which groups areunsubstituted or substituted by one or more groups selected from(C₁-C₄)alkoxy, S(O)_(n)R¹² and OH; or is —(CR⁹R¹⁰)_(p)R¹¹.
 3. A compoundor a salt thereof as claimed in claim 1, wherein R² is H,(C₃-C₆)alkenyl, (C₃-C₆)alkynyl, (C₁-C₆)alkoxy, (C₃-C₆)alkenyloxy,(C₃-C₆)alkynyloxy, —(CR⁹R¹⁰)_(p)R¹¹, —(CR⁹R¹⁰)_(p)heterocyclyl, NHR¹¹ orO(CH₂)_(n)R¹¹; or is (C₁-C₈)alkyl unsubstituted or substituted by adi-(C₁-C₄)alkylamino group.
 4. A compound or a salt thereof as claimedin claim 1, wherein R³ is (C₁-C₈)alkyl or (C₃-C₆)alkenyl, which groupsare unsubstituted or substituted by an (C₁-C₄)alkoxy or OH group; or isH or —(CR⁹R¹⁰)_(p)R¹¹.
 5. A compound or a salt thereof as claimed inclaim 1, wherein R⁴ is (C₁-C₈)alkyl substituted by (C₁-C₄)alkoxy or OH;or is (C₃-C₆)alkenyl, (C₃-₆)alkynyl or (C₃-C₈)cycloalkyl which lastthree mentioned groups are unsubstituted or substituted by an(C₁-C₄)alkoxy or OH group; or is (C₃-C₈)cycloalkyl-(C₁-C₆)alkyl whichcycloalkyl is unsubstituted or substituted by an (C₁-C₄)alkoxy or OHgroup; or is —(CR⁹R¹⁰)_(p)R¹¹ or —(CR⁹R¹⁰)_(p)heterocyclyl.
 6. Acompound or a salt thereof as claimed in claim 1, wherein N=Q is aformula (A) in which Z is YR¹ and R¹ and R³ form together with theadjacent —Y—C—NR²— atoms, a heterocyclic ring which is of formula (A¹),(A²), (A³) or (A⁴):

wherein: Y is O or S; U is N or CH; V is O or CH₂; t is 0 or 1; R^(a),R^(b), R^(c) and R^(d) are each independently selected from H,(C₁-C₆)alkyl, (C₁-C₆)haloalkyl, (C₂-C₆)alkenyl, (C₂-C₆)alkynyl,(C₃-C₈)cycloalkyl, halogen, (C₁-C₆)alkoxy, (C₁-C₆)haloalkoxy,S(O)_(n)R¹², (C₂-C₆)alkenyloxy, (C₂-C₆)alkynyloxy, R¹¹, heterocyclyl andO(CH₂)_(r)R¹¹ wherein r is 0 or 1; or R^(a) and R^(b), or R^(c) andR^(d) may form a carbonyl or imino group; R^(e) and R^(f) are eachindependently selected from H, (C₁-C₆)alkyl, (C₂-C₆)alkenyl,(C₂-C₆)alkynyl, (C₃-C₈)cycloalkyl, (C₃-C₈)cycloalkyl-(C₁-C₆)alkyl,halogen, (C₁-C₆)alkoxy, (C₁-C₆)haloalkoxy, S(O)_(n)R¹²,(C₂-C₆)alkenyloxy, (C₂-C₆)alkynyloxy, —(CH₂)_(p)R¹¹, heterocyclyl, CN,CO₂(C₁-C₆)alkyl, NO₂, amino, (C₁-C₆)alkylamino, di-(C₁-C₆)alkylamino andO(CH₂)_(r)R¹¹ wherein r is 0 or 1; R⁹ is H, (C₁-C₆)alkyl, halogen,(C₁-C₆)alkoxy, CO₂(C₁-C₆)alkyl or R¹¹; R^(2a) is (C₁-C₆)alkylunsubstituted or substituted by one or more groups selected fromhalogen, (C₁-C₆)alkoxy, CH[O(C₁-C₆)alkyl]₂, CN, CO₂(C₁-C₆)alkyl andCO₂H; or is (C₃-C₆)alkenyl unsubstituted or substituted by one or morehalogen or phenyl groups; or is (C₃-C₆)alkynyl, (C₃-C₈)cycloalkyl,(C₃-C₈)cycloalkyl-(C₁-C₆)alkyl, (C₁-C₆)alkoxy, (C₃-C₆)alkenyloxy or(C₃-C₆)alkynyloxy; or is —(CHR₁₀)_(p)R¹¹ wherein R¹⁰ is H or(C₁-C₈)alkyl, p is 0 or 1 and R¹¹ is phenyl unsubstituted or substitutedby one or more groups selected from halogen, (C₁-C₆)haloalkyl,(C₁-C₆)alkoxy, (C₁-C₆)haloalkoxy and phenoxy unsubstituted orsubstituted by one or more groups selected from halogen and(C₁-C₆)haloalkyl; or is O(CHR¹⁰)_(r)R¹¹ wherein R₁₁ is H or(C₁-C₆)alkyl, r is 1 and R¹¹ is phenyl unsubstituted or substituted byone or more groups selected from (C₁-C₆)haloalkyl, (C₁-C₆)alkoxy andNO₂; and R² is R^(2a) or H.
 7. A compound or salt thereof as claimed inclaim 1, wherein R¹ is (C₁-C₈)alkyl or (C₃-C₆)alkenyl, which groups areunsubstituted or substituted by one or more groups selected from(C₁-C₄)alkoxy, S(O)_(n)R¹² and OH; or is —(CR⁹R¹⁰)_(p)R¹¹.
 8. A compoundor salt thereof as claimed in claim 1, wherein R² is H, (C₃-C₆)alkenyl,(C₃-C₆)alkynyl, (C₁-C₆)alkoxy, (C₃-C₆)alkenyloxy, (C₃-C₆)alkynyloxy,—(CR⁹R¹⁰)_(p)R¹¹, —(CR⁹R¹⁰)_(p)heterocyclyl, NHR¹¹ or O(CH₂)_(r)R¹¹; oris (C₁-C₈)alkyl unsubstituted or substituted by a di-(C₁-C₄)alkylaminogroup.
 9. A compound or salt thereof as claimed in claim 2, wherein R²is H, (C₃-C₆)alkenyl, (C₃-C₆)alkynyl, (C₁-C₆)alkoxy, (C₃-C₆)alkenyloxy,(C₃-C₆)alkynyloxy, —(CR⁹R¹⁰)_(p)R¹¹, —(CR⁹R¹⁰)_(p)heterocyclyl, NHR¹¹ orO(CH₂)_(r)R¹¹; or is (C₁-C₈)alkyl unsubstituted or substituted by adi-(C₁-C₄)alkylamino group.
 10. A compound or salt thereof as claimed inclaim 1, wherein R³ is (C₁-C₈)alkyl or (C₃-C₆)alkenyl, which groups areunsubstituted or substituted by an (C₁-C₄)alkoxy or OH group; or is H or—(CR⁹R¹⁰)_(p)R¹¹.
 11. A compound or salt thereof as claimed in claim 2,wherein R³ is (C₁-C₈)alkyl or (C₃-C₆)alkenyl, which groups areunsubstituted or substituted by an (C₁-C₄)alkoxy or OH group; or is H or—(CR⁹R¹⁰)_(p)R¹¹.
 12. A compound or salt thereof as claimed in claim 3,wherein R³ is (C₁-C₈)alkyl or (C₃-C₆)alkenyl, which groups areunsubstituted or substituted by an (C₁-C₄)alkoxy or OH group; or is H or—(CR⁹R¹⁰)_(p)R¹¹.
 13. A compound or salt thereof as claimed in claim 1,wherein R⁴ is (C₁-C₈)alkyl substituted by (C₁-C₄)alkoxy or OH; or is(C₃-C₆)alkenyl, (C₃-C₆)alkynyl or (C₃-C₈)cycloalkyl which last threementioned groups are unsubstituted or substituted by an (C₁-C₄)alkoxy orOH group; or is (C₃-C₈)cycloalkyl-(C₁-C₆)alkyl which cycloalkyl isunsubstituted or substituted by an (C₁-C₄)alkoxy or OH group; or is—(CR⁹R¹⁰)_(p)R¹¹ or —(CR⁹R¹⁰)_(p)heterocyclyl.
 14. A compound or saltthereof as claimed in claim 2, wherein R⁴ is (C₁-C₈)alkyl substituted by(C₁-C₄)alkoxy or OH; or is (C₃-C₆)alkenyl, (C₃-C₆)alkynyl or(C₃-C₈)cycloalkyl which last three mentioned groups are unsubstituted orsubstituted by an (C₁-C₄)alkoxy or OH group; or is(C₃-C₈)cycloalkyl-(C₁-C₆)alkyl which cycloalkyl is unsubstituted orsubstituted by an (C₁-C₄)alkoxy or OH group; or is —(CR⁹R¹⁰)_(p)R¹¹ or—(CR⁹R¹⁰)_(p)heterocyclyl.
 15. A compound or salt thereof as claimed inclaim 3, wherein R⁴ is (C₁-C₈)alkyl substituted by (C₁-C₄)alkoxy or OH;or is (C₃-C₆)alkenyl, (C₃-C₆)alkynyl or (C₃-C₈)cycloalkyl which lastthree mentioned groups are unsubstituted or substituted by an(C₁-C₄)alkoxy or OH group; or is (C₃-C₈)cycloalkyl-(C₁-C₆)alkyl whichcycloalkyl is unsubstituted or substituted by an (C₁-C₄)alkoxy or OHgroup; or is —(CR⁹R¹⁰)_(p)R¹¹ or —(CR⁹R¹⁰)_(p)heterocyclyl.
 16. Acompound or salt thereof as claimed in claim 4, wherein R⁴ is(C₁-C₈)alkyl substituted by (C₁-C₄)alkoxy or OH; or is (C₃-C₆)alkenyl,(C₃-C₆)alkynyl or (C₃-C₈)cycloalkyl which last three mentioned groupsare unsubstituted or substituted by an (C₁-C₄)alkoxy or OH group; or is(C₃-C₈)cycloalkyl-(C₁-C₆)alkyl which cycloalkyl is unsubstituted orsubstituted by an (C₁-C₄)alkoxy or OH group; or is —(CR⁹R¹⁰)_(p)R¹¹ or—(CR⁹R¹⁰)_(p)heterocyclyl.
 17. A pesticidal composition comprising apesticidally effective amount of a compound of formula (I) or apesticidally acceptable salt thereof as defined in claim 1, inassociation with a pesticidally acceptable diluent or carrier and/orsurface active agent.
 18. A method for the control of arthropod ornematode pests, said method comprising applying to said pests or to alocus at which they reside or feed or which is susceptible toinfestation thereby, a pesticidally effective amount of a compound orsalt thereof as claimed in claim
 1. 19. A method for the control ofarthropod or nematode pests, said method comprising applying to saidpests or to a locus at which they reside or feed or which is susceptibleto infestation thereby, a pesticidally effective amount of a compositionas claimed in claim
 17. 20. A process for the preparation of a compoundof formula (I)

or a salt thereof as defined in claim 6, which process comprises: a)where N=Q is a formula (A) in which Z is YR¹, m is zero, and R¹, R² andR³ are as defined in claim 6, reacting a compound of formula (II):

wherein Y, R² and R³ are as defined in formula (I), with a compound offormula (III):R¹L  (III) wherein R¹ is as defined in formula (I) and L is a leavinggroup in the presence of a base; or b) where N=Q is a formula (A) inwhich Z is YR¹, m is zero, R³ is H, and R¹ and R² are as defined informula (I), as a 1-pot reaction, reacting a compound of formula (IV):

with a strong base, and an isothiocyanate or isocyanate compound offormula (V):R²—N═C═Y  (V) wherein R² is as defined in formula (I) to give thecorresponding acylthiourea or acylurea intermediate of formula (II)above wherein R³ is H, followed by reacting said intermediate with acompound of formula (III) as described in above process a); or c) whereN=Q is a formula (A) which is a heterocyclic ring of formula (A¹), (A²),(A³) or (A⁴), wherein the various symbols are as defined in claim 6,acylating the corresponding compound of formula (A^(1a)), (A^(2a)),(A^(3a)) or (A^(4a)):

wherein the various symbols are as defined in claim 6, with a compoundof formula (VI):

wherein L is a leaving group; or d) where N=Q is a formula (A) which isa heterocyclic ring of formula (A¹) or (A⁴), m is zero, Y is S and theother symbols are as defined in claim 6, cyclizing a compound of formula(IX) or (X) respectively:

wherein the various symbols are as defined in formula (I) and L₁ is aleaving group, in the presence of a base; or e) where m is zero and N=Qis a formula (B) in which R¹ and R⁴ are as defined in formula (I), thereaction of reacting a compound of formula (XI):

wherein X, W and R⁴ are as defined in formula (I), with a compound offormula (III) as defined in the above process a), in the presence of abase; or f) where Q is as defined above, and m is 1 oxidizing acorresponding compound in which m is 0; and if desired, converting aresulting compound of formula (I) into a pesticidally acceptable saltthereof.